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SKI-606 (Bosutinib) inhibiteur de Src/Abl

Name: SKI-606 (Bosutinib)
Brand: Selleck Chemicals
SKU: S1014
Rating: 5 (146 reviews)

Réf. CatalogueS1014

Le Bosutinib est un nouvel inhibiteur double Src/Abl, avec des IC50 de 1,2 nM et 1 nM respectivement dans les essais acellulaires. Le Bosutinib diminue également efficacement l'activité des voies de signalisation PI3K/AKT/mTOR, MAPK/ERK et JAK/STAT3 en bloquant les niveaux de phosphorylation de p-ERK, p-S6 et p-STAT3. Le Bosutinib favorise l'autophagy.

SKI-606 (Bosutinib) Src inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 530.45

Aller à

Contrôle Qualité

Lot : Pureté : 99.94%

99.94

Cibles apparentées	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Autre Src Inhibiteurs	WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité	PMID
NB7	Growth Inhibition Assay		IC50=0.08231 μM	SANGER
SW756	Growth Inhibition Assay		IC50=0.14024 μM	SANGER
CTV-1	Growth Inhibition Assay		IC50=0.16398 μM	SANGER
HSC-4	Growth Inhibition Assay		IC50=0.17158 μM	SANGER
LAMA-84	Growth Inhibition Assay		IC50=0.28664 μM	SANGER
KU812	Growth Inhibition Assay		IC50=0.34068 μM	SANGER
HCC1806	Growth Inhibition Assay		IC50=0.35216 μM	SANGER
DOK	Growth Inhibition Assay		IC50=0.37786 μM	SANGER
NCI-H209	Growth Inhibition Assay		IC50=0.40808 μM	SANGER
EoL-1-cell	Growth Inhibition Assay		IC50=0.41576 μM	SANGER
H9	Growth Inhibition Assay		IC50=0.43464 μM	SANGER
EM-2	Growth Inhibition Assay		IC50=0.4389 μM	SANGER
NCI-H292	Growth Inhibition Assay		IC50=0.44108 μM	SANGER
697	Growth Inhibition Assay		IC50=0.45633 μM	SANGER
BHT-101	Growth Inhibition Assay		IC50=0.4659 μM	SANGER
BE-13	Growth Inhibition Assay		IC50=0.48572 μM	SANGER
RS4-11	Growth Inhibition Assay		IC50=0.48584 μM	SANGER
IGROV-1	Growth Inhibition Assay		IC50=0.48797 μM	SANGER
KE-37	Growth Inhibition Assay		IC50=0.49509 μM	SANGER
BV-173	Growth Inhibition Assay		IC50=0.50792 μM	SANGER
MEG-01	Growth Inhibition Assay		IC50=0.51214 μM	SANGER
LB2241-RCC	Growth Inhibition Assay		IC50=0.53718 μM	SANGER
ACHN	Growth Inhibition Assay		IC50=0.54069 μM	SANGER
CTB-1	Growth Inhibition Assay		IC50=0.5482 μM	SANGER
HT-1080	Growth Inhibition Assay		IC50=0.55349 μM	SANGER
CHL-1	Growth Inhibition Assay		IC50=0.55465 μM	SANGER
EW-3	Growth Inhibition Assay		IC50=0.55935 μM	SANGER
ES1	Growth Inhibition Assay		IC50=0.67498 μM	SANGER
KASUMI-1	Growth Inhibition Assay		IC50=0.7233 μM	SANGER
SW13	Growth Inhibition Assay		IC50=0.73798 μM	SANGER
A3-KAW	Growth Inhibition Assay		IC50=0.79208 μM	SANGER
LB771-HNC	Growth Inhibition Assay		IC50=0.83104 μM	SANGER
OC-314	Growth Inhibition Assay		IC50=0.86965 μM	SANGER
MLMA	Growth Inhibition Assay		IC50=0.90675 μM	SANGER
KARPAS-45	Growth Inhibition Assay		IC50=0.92466 μM	SANGER
CAL-27	Growth Inhibition Assay		IC50=0.92906 μM	SANGER
SK-NEP-1	Growth Inhibition Assay		IC50=0.97248 μM	SANGER
COR-L105	Growth Inhibition Assay		IC50=1.00394 μM	SANGER
TI-73	Growth Inhibition Assay		IC50=1.0165 μM	SANGER
JVM-3	Growth Inhibition Assay		IC50=1.05017 μM	SANGER
HAL-01	Growth Inhibition Assay		IC50=1.0881 μM	SANGER
QIMR-WIL	Growth Inhibition Assay		IC50=1.09058 μM	SANGER
HSC-3	Growth Inhibition Assay		IC50=1.11783 μM	SANGER
KY821	Growth Inhibition Assay		IC50=1.13351 μM	SANGER
5637	Growth Inhibition Assay		IC50=1.13803 μM	SANGER
CAL-33	Growth Inhibition Assay		IC50=1.19302 μM	SANGER
ES4	Growth Inhibition Assay		IC50=1.2079 μM	SANGER
BHY	Growth Inhibition Assay		IC50=1.22892 μM	SANGER
LB1047-RCC	Growth Inhibition Assay		IC50=1.23785 μM	SANGER
H4	Growth Inhibition Assay		IC50=1.24255 μM	SANGER
RPMI-8866	Growth Inhibition Assay		IC50=1.26106 μM	SANGER
HO-1-N-1	Growth Inhibition Assay		IC50=1.26369 μM	SANGER
BB30-HNC	Growth Inhibition Assay		IC50=1.28714 μM	SANGER
PC-14	Growth Inhibition Assay		IC50=1.29205 μM	SANGER
NUGC-3	Growth Inhibition Assay		IC50=1.29356 μM	SANGER
A4-Fuk	Growth Inhibition Assay		IC50=1.30704 μM	SANGER
MHH-NB-11	Growth Inhibition Assay		IC50=1.31383 μM	SANGER
KOSC-2	Growth Inhibition Assay		IC50=1.31775 μM	SANGER
A498	Growth Inhibition Assay		IC50=1.40113 μM	SANGER
KG-1	Growth Inhibition Assay		IC50=1.41273 μM	SANGER
DEL	Growth Inhibition Assay		IC50=1.43657 μM	SANGER
EW-16	Growth Inhibition Assay		IC50=1.43973 μM	SANGER
BPH-1	Growth Inhibition Assay		IC50=1.44805 μM	SANGER
JAR	Growth Inhibition Assay		IC50=1.4936 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay		IC50=1.51722 μM	SANGER
A375	Growth Inhibition Assay		IC50=1.51772 μM	SANGER
SW954	Growth Inhibition Assay		IC50=1.55007 μM	SANGER
Ca9-22	Growth Inhibition Assay		IC50=1.5626 μM	SANGER
D-566MG	Growth Inhibition Assay		IC50=1.57155 μM	SANGER
SCC-15	Growth Inhibition Assay		IC50=1.61804 μM	SANGER
HD-MY-Z	Growth Inhibition Assay		IC50=1.63584 μM	SANGER
HT-1376	Growth Inhibition Assay		IC50=1.6436 μM	SANGER
CAL-54	Growth Inhibition Assay		IC50=1.65709 μM	SANGER
ONS-76	Growth Inhibition Assay		IC50=1.67551 μM	SANGER
EFO-27	Growth Inhibition Assay		IC50=1.6892 μM	SANGER
769-P	Growth Inhibition Assay		IC50=1.69596 μM	SANGER
MV-4-11	Growth Inhibition Assay		IC50=1.69856 μM	SANGER
NKM-1	Growth Inhibition Assay		IC50=1.71802 μM	SANGER
LOXIMVI	Growth Inhibition Assay		IC50=1.74599 μM	SANGER
KYSE-140	Growth Inhibition Assay		IC50=1.75655 μM	SANGER
ES5	Growth Inhibition Assay		IC50=1.86747 μM	SANGER
BB65-RCC	Growth Inhibition Assay		IC50=1.89849 μM	SANGER
HN	Growth Inhibition Assay		IC50=1.89874 μM	SANGER
A101D	Growth Inhibition Assay		IC50=1.93628 μM	SANGER
LoVo	Growth Inhibition Assay		IC50=1.97679 μM	SANGER
NCI-H526	Growth Inhibition Assay		IC50=1.99325 μM	SANGER
NCI-H1693	Growth Inhibition Assay		IC50=1.99888 μM	SANGER
OVCAR-4	Growth Inhibition Assay		IC50=2.00435 μM	SANGER
SK-HEP-1	Growth Inhibition Assay		IC50=2.00745 μM	SANGER
C2BBe1	Growth Inhibition Assay		IC50=2.03372 μM	SANGER
MEL-JUSO	Growth Inhibition Assay		IC50=2.04464 μM	SANGER
MOLT-16	Growth Inhibition Assay		IC50=2.07058 μM	SANGER
NBsusSR	Growth Inhibition Assay		IC50=2.09889 μM	SANGER
TK10	Growth Inhibition Assay		IC50=2.13458 μM	SANGER
CAL-39	Growth Inhibition Assay		IC50=2.1448 μM	SANGER
NCI-H2030	Growth Inhibition Assay		IC50=2.18973 μM	SANGER
HCT-116	Growth Inhibition Assay		IC50=2.22984 μM	SANGER
HTC-C3	Growth Inhibition Assay		IC50=2.26824 μM	SANGER
TYK-nu	Growth Inhibition Assay		IC50=2.30909 μM	SANGER
FADU	Growth Inhibition Assay		IC50=2.32296 μM	SANGER
A431	Growth Inhibition Assay		IC50=2.37025 μM	SANGER
TE-11	Growth Inhibition Assay		IC50=2.38019 μM	SANGER
CAL-12T	Growth Inhibition Assay		IC50=2.40417 μM	SANGER
DB	Growth Inhibition Assay		IC50=2.42869 μM	SANGER
L-363	Growth Inhibition Assay		IC50=2.43507 μM	SANGER
MSTO-211H	Growth Inhibition Assay		IC50=2.66391 μM	SANGER
SK-UT-1	Growth Inhibition Assay		IC50=2.71406 μM	SANGER
RPMI-8226	Growth Inhibition Assay		IC50=2.73164 μM	SANGER
SF295	Growth Inhibition Assay		IC50=2.7431 μM	SANGER
OS-RC-2	Growth Inhibition Assay		IC50=2.76673 μM	SANGER
SK-MEL-24	Growth Inhibition Assay		IC50=2.78224 μM	SANGER
COR-L23	Growth Inhibition Assay		IC50=2.79464 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay		IC50=2.80161 μM	SANGER
SK-N-DZ	Growth Inhibition Assay		IC50=2.81638 μM	SANGER
OMC-1	Growth Inhibition Assay		IC50=2.85003 μM	SANGER
SK-MEL-2	Growth Inhibition Assay		IC50=2.89243 μM	SANGER
SAS	Growth Inhibition Assay		IC50=2.99415 μM	SANGER
EPLC-272H	Growth Inhibition Assay		IC50=3.00235 μM	SANGER
8505C	Growth Inhibition Assay		IC50=3.10301 μM	SANGER
EW-11	Growth Inhibition Assay		IC50=3.14277 μM	SANGER
YKG-1	Growth Inhibition Assay		IC50=3.14706 μM	SANGER
EC-GI-10	Growth Inhibition Assay		IC50=3.17263 μM	SANGER
SK-LU-1	Growth Inhibition Assay		IC50=3.18418 μM	SANGER
P30-OHK	Growth Inhibition Assay		IC50=3.20117 μM	SANGER
T-24	Growth Inhibition Assay		IC50=3.21814 μM	SANGER
HSC-2	Growth Inhibition Assay		IC50=3.22232 μM	SANGER
SK-MES-1	Growth Inhibition Assay		IC50=3.24829 μM	SANGER
SW48	Growth Inhibition Assay		IC50=3.25486 μM	SANGER
ME-180	Growth Inhibition Assay		IC50=3.26051 μM	SANGER
NCI-H2009	Growth Inhibition Assay		IC50=3.2901 μM	SANGER
HL-60	Growth Inhibition Assay		IC50=3.2913 μM	SANGER
NCI-N87	Growth Inhibition Assay		IC50=3.30172 μM	SANGER
GMS-10	Growth Inhibition Assay		IC50=3.34086 μM	SANGER
SCH	Growth Inhibition Assay		IC50=3.40844 μM	SANGER
C-33-A	Growth Inhibition Assay		IC50=3.41421 μM	SANGER
NCI-H1703	Growth Inhibition Assay		IC50=3.41812 μM	SANGER
A427	Growth Inhibition Assay		IC50=3.46124 μM	SANGER
MOLT-4	Growth Inhibition Assay		IC50=3.48199 μM	SANGER
NCI-H1792	Growth Inhibition Assay		IC50=3.49802 μM	SANGER
NCI-H1650	Growth Inhibition Assay		IC50=3.5729 μM	SANGER
H-EMC-SS	Growth Inhibition Assay		IC50=3.58569 μM	SANGER
SW982	Growth Inhibition Assay		IC50=3.58829 μM	SANGER
DSH1	Growth Inhibition Assay		IC50=3.64122 μM	SANGER
NOS-1	Growth Inhibition Assay		IC50=3.64276 μM	SANGER
BT-549	Growth Inhibition Assay		IC50=3.67854 μM	SANGER
HuCCT1	Growth Inhibition Assay		IC50=3.74177 μM	SANGER
NCI-H1755	Growth Inhibition Assay		IC50=3.96971 μM	SANGER
KYSE-450	Growth Inhibition Assay		IC50=3.96997 μM	SANGER
MIA-PaCa-2	Growth Inhibition Assay		IC50=3.9729 μM	SANGER
U-266	Growth Inhibition Assay		IC50=3.97481 μM	SANGER
Mewo	Growth Inhibition Assay		IC50=4.06361 μM	SANGER
KYSE-520	Growth Inhibition Assay		IC50=4.09799 μM	SANGER
MN-60	Growth Inhibition Assay		IC50=4.10501 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay		IC50=4.16739 μM	SANGER
SK-MEL-1	Growth Inhibition Assay		IC50=4.18695 μM	SANGER
ABC-1	Growth Inhibition Assay		IC50=4.23333 μM	SANGER
CAKI-1	Growth Inhibition Assay		IC50=4.24571 μM	SANGER
HOS	Growth Inhibition Assay		IC50=4.29141 μM	SANGER
SN12C	Growth Inhibition Assay		IC50=4.34244 μM	SANGER
NB13	Growth Inhibition Assay		IC50=4.37355 μM	SANGER
M14	Growth Inhibition Assay		IC50=4.48792 μM	SANGER
GP5d	Growth Inhibition Assay		IC50=4.5012 μM	SANGER
NCI-H720	Growth Inhibition Assay		IC50=4.53612 μM	SANGER
D-423MG	Growth Inhibition Assay		IC50=4.53924 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay		IC50=4.59559 μM	SANGER
MEL-HO	Growth Inhibition Assay		IC50=4.61261 μM	SANGER
MHH-ES-1	Growth Inhibition Assay		IC50=4.62411 μM	SANGER
KYSE-270	Growth Inhibition Assay		IC50=4.65126 μM	SANGER
GI-ME-N	Growth Inhibition Assay		IC50=4.71291 μM	SANGER
HOP-92	Growth Inhibition Assay		IC50=4.81379 μM	SANGER
MKN1	Growth Inhibition Assay		IC50=4.83914 μM	SANGER
ML-2	Growth Inhibition Assay		IC50=4.85626 μM	SANGER
RO82-W-1	Growth Inhibition Assay		IC50=4.9298 μM	SANGER
G-361	Growth Inhibition Assay		IC50=5.01003 μM	SANGER
HC-1	Growth Inhibition Assay		IC50=5.03291 μM	SANGER
EW-24	Growth Inhibition Assay		IC50=5.04038 μM	SANGER
HuP-T4	Growth Inhibition Assay		IC50=5.14334 μM	SANGER
8-MG-BA	Growth Inhibition Assay		IC50=5.3428 μM	SANGER
HGC-27	Growth Inhibition Assay		IC50=5.37682 μM	SANGER
TE-12	Growth Inhibition Assay		IC50=5.41585 μM	SANGER
GT3TKB	Growth Inhibition Assay		IC50=5.44212 μM	SANGER
DOHH-2	Growth Inhibition Assay		IC50=5.45986 μM	SANGER
Ca-Ski	Growth Inhibition Assay		IC50=5.46115 μM	SANGER
A172	Growth Inhibition Assay		IC50=5.54925 μM	SANGER
EGI-1	Growth Inhibition Assay		IC50=5.58938 μM	SANGER
MZ2-MEL	Growth Inhibition Assay		IC50=5.61486 μM	SANGER
SW1710	Growth Inhibition Assay		IC50=5.69091 μM	SANGER
HT-144	Growth Inhibition Assay		IC50=5.72685 μM	SANGER
PA-1	Growth Inhibition Assay		IC50=5.81893 μM	SANGER
HCC1937	Growth Inhibition Assay		IC50=5.83929 μM	SANGER
SK-OV-3	Growth Inhibition Assay		IC50=5.91121 μM	SANGER
K5	Growth Inhibition Assay		IC50=6.0517 μM	SANGER
NMC-G1	Growth Inhibition Assay		IC50=6.07797 μM	SANGER
MDA-MB-361	Growth Inhibition Assay		IC50=6.09261 μM	SANGER
EKVX	Growth Inhibition Assay		IC50=6.13501 μM	SANGER
ES7	Growth Inhibition Assay		IC50=6.16115 μM	SANGER
KS-1	Growth Inhibition Assay		IC50=6.17993 μM	SANGER
NCI-H661	Growth Inhibition Assay		IC50=6.18081 μM	SANGER
ES8	Growth Inhibition Assay		IC50=6.18082 μM	SANGER
NCI-H23	Growth Inhibition Assay		IC50=6.21816 μM	SANGER
T47D	Growth Inhibition Assay		IC50=6.26457 μM	SANGER
A2780	Growth Inhibition Assay		IC50=6.37701 μM	SANGER
SCC-4	Growth Inhibition Assay		IC50=6.43561 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay		IC50=6.97043 μM	SANGER
no-11	Growth Inhibition Assay		IC50=7.1641 μM	SANGER
KU-19-19	Growth Inhibition Assay		IC50=7.16476 μM	SANGER
MKN45	Growth Inhibition Assay		IC50=7.18699 μM	SANGER
SCC-25	Growth Inhibition Assay		IC50=7.23414 μM	SANGER
ETK-1	Growth Inhibition Assay		IC50=7.25514 μM	SANGER
COR-L88	Growth Inhibition Assay		IC50=7.29319 μM	SANGER
8305C	Growth Inhibition Assay		IC50=7.32492 μM	SANGER
Detroit562	Growth Inhibition Assay		IC50=7.32506 μM	SANGER
SNU-449	Growth Inhibition Assay		IC50=7.37651 μM	SANGER
A704	Growth Inhibition Assay		IC50=7.38278 μM	SANGER
D-502MG	Growth Inhibition Assay		IC50=7.38473 μM	SANGER
NCI-H2228	Growth Inhibition Assay		IC50=7.41458 μM	SANGER
CHP-212	Growth Inhibition Assay		IC50=7.51896 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay		IC50=7.59066 μM	SANGER
RPMI-2650	Growth Inhibition Assay		IC50=7.70312 μM	SANGER
HCC2218	Growth Inhibition Assay		IC50=7.72258 μM	SANGER
GCT	Growth Inhibition Assay		IC50=7.82172 μM	SANGER
SW780	Growth Inhibition Assay		IC50=7.9906 μM	SANGER
KMOE-2	Growth Inhibition Assay		IC50=8.0407 μM	SANGER
KYSE-180	Growth Inhibition Assay		IC50=8.08648 μM	SANGER
TE-1	Growth Inhibition Assay		IC50=8.11057 μM	SANGER
OAW-42	Growth Inhibition Assay		IC50=8.25496 μM	SANGER
VM-CUB-1	Growth Inhibition Assay		IC50=8.28364 μM	SANGER
ECC10	Growth Inhibition Assay		IC50=8.28397 μM	SANGER
SW1573	Growth Inhibition Assay		IC50=8.44465 μM	SANGER
NCI-H1299	Growth Inhibition Assay		IC50=8.59774 μM	SANGER
ALL-PO	Growth Inhibition Assay		IC50=8.66597 μM	SANGER
OVCAR-5	Growth Inhibition Assay		IC50=8.77625 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay		IC50=8.83001 μM	SANGER
NCI-H2342	Growth Inhibition Assay		IC50=8.83101 μM	SANGER
RPMI-7951	Growth Inhibition Assay		IC50=8.84157 μM	SANGER
RCM-1	Growth Inhibition Assay		IC50=9.08145 μM	SANGER
Daoy	Growth Inhibition Assay		IC50=9.12028 μM	SANGER
HCC1395	Growth Inhibition Assay		IC50=9.30896 μM	SANGER
786-0	Growth Inhibition Assay		IC50=9.36026 μM	SANGER
GAMG	Growth Inhibition Assay		IC50=9.65534 μM	SANGER
HCC1954	Growth Inhibition Assay		IC50=9.85859 μM	SANGER
NCI-H1838	Growth Inhibition Assay		IC50=9.90371 μM	SANGER
SW620	Growth Inhibition Assay		IC50=9.95357 μM	SANGER
NCI-H358	Growth Inhibition Assay		IC50=10.4197 μM	SANGER
NCI-H1793	Growth Inhibition Assay		IC50=10.4248 μM	SANGER
NCI-H1666	Growth Inhibition Assay		IC50=10.4355 μM	SANGER
MZ7-mel	Growth Inhibition Assay		IC50=10.4753 μM	SANGER
MDA-MB-175-VII	Growth Inhibition Assay		IC50=10.6396 μM	SANGER
COLO-829	Growth Inhibition Assay		IC50=10.8004 μM	SANGER
RVH-421	Growth Inhibition Assay		IC50=11.152 μM	SANGER
A549	Growth Inhibition Assay		IC50=11.2478 μM	SANGER
DJM-1	Growth Inhibition Assay		IC50=11.3833 μM	SANGER
IST-MEL1	Growth Inhibition Assay		IC50=11.7319 μM	SANGER
BEN	Growth Inhibition Assay		IC50=11.7402 μM	SANGER
KM12	Growth Inhibition Assay		IC50=11.9091 μM	SANGER
HuO9	Growth Inhibition Assay		IC50=12.0666 μM	SANGER
U-2-OS	Growth Inhibition Assay		IC50=12.0893 μM	SANGER
RH-1	Growth Inhibition Assay		IC50=12.4472 μM	SANGER
NCI-H1048	Growth Inhibition Assay		IC50=12.5506 μM	SANGER
Mo-T	Growth Inhibition Assay		IC50=12.7307 μM	SANGER
KYSE-150	Growth Inhibition Assay		IC50=12.7455 μM	SANGER
A388	Growth Inhibition Assay		IC50=12.7713 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay		IC50=12.8046 μM	SANGER
HEL	Growth Inhibition Assay		IC50=12.8212 μM	SANGER
UM-UC-3	Growth Inhibition Assay		IC50=12.8874 μM	SANGER
TGBC24TKB	Growth Inhibition Assay		IC50=13.0267 μM	SANGER
SW626	Growth Inhibition Assay		IC50=13.2485 μM	SANGER
ES6	Growth Inhibition Assay		IC50=13.2512 μM	SANGER
NCI-H2029	Growth Inhibition Assay		IC50=13.8108 μM	SANGER
RXF393	Growth Inhibition Assay		IC50=13.9927 μM	SANGER
HMV-II	Growth Inhibition Assay		IC50=14.078 μM	SANGER
EW-22	Growth Inhibition Assay		IC50=14.1502 μM	SANGER
AsPC-1	Growth Inhibition Assay		IC50=14.564 μM	SANGER
COLO-678	Growth Inhibition Assay		IC50=14.7271 μM	SANGER
HCT-15	Growth Inhibition Assay		IC50=14.8855 μM	SANGER
HCE-T	Growth Inhibition Assay		IC50=14.8874 μM	SANGER
SF539	Growth Inhibition Assay		IC50=15.0643 μM	SANGER
AU565	Growth Inhibition Assay		IC50=15.2096 μM	SANGER
JVM-2	Growth Inhibition Assay		IC50=15.2681 μM	SANGER
CaR-1	Growth Inhibition Assay		IC50=15.4412 μM	SANGER
23132-87	Growth Inhibition Assay		IC50=15.8495 μM	SANGER
A673	Growth Inhibition Assay		IC50=15.9636 μM	SANGER
KYSE-410	Growth Inhibition Assay		IC50=16.029 μM	SANGER
TE-9	Growth Inhibition Assay		IC50=16.062 μM	SANGER
LU-139	Growth Inhibition Assay		IC50=16.1823 μM	SANGER
GCIY	Growth Inhibition Assay		IC50=16.1916 μM	SANGER
JEG-3	Growth Inhibition Assay		IC50=16.25 μM	SANGER
RT-112	Growth Inhibition Assay		IC50=16.4143 μM	SANGER
COLO-680N	Growth Inhibition Assay		IC50=16.5108 μM	SANGER
LU-134-A	Growth Inhibition Assay		IC50=16.9893 μM	SANGER
MFM-223	Growth Inhibition Assay		IC50=17.1535 μM	SANGER
SF126	Growth Inhibition Assay		IC50=17.1701 μM	SANGER
NCI-H28	Growth Inhibition Assay		IC50=17.2066 μM	SANGER
BFTC-905	Growth Inhibition Assay		IC50=17.4832 μM	SANGER
SCC-9	Growth Inhibition Assay		IC50=17.6285 μM	SANGER
KNS-62	Growth Inhibition Assay		IC50=17.6629 μM	SANGER
Hs-578-T	Growth Inhibition Assay		IC50=17.8149 μM	SANGER
D-336MG	Growth Inhibition Assay		IC50=17.8294 μM	SANGER
NCI-H82	Growth Inhibition Assay		IC50=18.0183 μM	SANGER
EFM-19	Growth Inhibition Assay		IC50=18.0577 μM	SANGER
TGBC11TKB	Growth Inhibition Assay		IC50=18.1021 μM	SANGER
HEC-1	Growth Inhibition Assay		IC50=18.2918 μM	SANGER
HuP-T3	Growth Inhibition Assay		IC50=18.5929 μM	SANGER
SF268	Growth Inhibition Assay		IC50=18.6702 μM	SANGER
COLO-792	Growth Inhibition Assay		IC50=18.7997 μM	SANGER
HLE	Growth Inhibition Assay		IC50=18.8331 μM	SANGER
A204	Growth Inhibition Assay		IC50=18.9164 μM	SANGER
CAL-72	Growth Inhibition Assay		IC50=19.0877 μM	SANGER
U031	Growth Inhibition Assay		IC50=19.4909 μM	SANGER
FTC-133	Growth Inhibition Assay		IC50=19.9304 μM	SANGER
SK-MEL-28	Growth Inhibition Assay		IC50=20.3761 μM	SANGER
KGN	Growth Inhibition Assay		IC50=20.4699 μM	SANGER
HCC2998	Growth Inhibition Assay		IC50=21.3926 μM	SANGER
GOTO	Growth Inhibition Assay		IC50=21.485 μM	SANGER
AGS	Growth Inhibition Assay		IC50=21.8451 μM	SANGER
EW-13	Growth Inhibition Assay		IC50=22.1022 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay		IC50=22.1603 μM	SANGER
NCI-H1395	Growth Inhibition Assay		IC50=22.2907 μM	SANGER
A2058	Growth Inhibition Assay		IC50=22.434 μM	SANGER
SH-4	Growth Inhibition Assay		IC50=22.7045 μM	SANGER
DoTc2-4510	Growth Inhibition Assay		IC50=23.6472 μM	SANGER
MMAC-SF	Growth Inhibition Assay		IC50=23.6911 μM	SANGER
NCI-H510A	Growth Inhibition Assay		IC50=23.7939 μM	SANGER
HDLM-2	Growth Inhibition Assay		IC50=24.146 μM	SANGER
KINGS-1	Growth Inhibition Assay		IC50=24.242 μM	SANGER
NCI-H1648	Growth Inhibition Assay		IC50=24.4024 μM	SANGER
HCC1187	Growth Inhibition Assay		IC50=25.0235 μM	SANGER
BALL-1	Growth Inhibition Assay		IC50=25.2062 μM	SANGER
SBC-1	Growth Inhibition Assay		IC50=25.2993 μM	SANGER
BFTC-909	Growth Inhibition Assay		IC50=25.3551 μM	SANGER
MOLT-13	Growth Inhibition Assay		IC50=25.6744 μM	SANGER
SW1990	Growth Inhibition Assay		IC50=25.9655 μM	SANGER
DK-MG	Growth Inhibition Assay		IC50=26.0443 μM	SANGER
TE-8	Growth Inhibition Assay		IC50=26.0668 μM	SANGER
Becker	Growth Inhibition Assay		IC50=26.1574 μM	SANGER
KYSE-70	Growth Inhibition Assay		IC50=26.5317 μM	SANGER
MKN7	Growth Inhibition Assay		IC50=27.7479 μM	SANGER
D-392MG	Growth Inhibition Assay		IC50=27.7694 μM	SANGER
NH-12	Growth Inhibition Assay		IC50=28.1229 μM	SANGER
EW-18	Growth Inhibition Assay		IC50=28.2218 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay		IC50=28.2762 μM	SANGER
NCI-H1770	Growth Inhibition Assay		IC50=28.3566 μM	SANGER
BT-20	Growth Inhibition Assay		IC50=28.3685 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay		IC50=28.4838 μM	SANGER
HPAF-II	Growth Inhibition Assay		IC50=28.779 μM	SANGER
SW837	Growth Inhibition Assay		IC50=29.3385 μM	SANGER
647-V	Growth Inhibition Assay		IC50=29.7003 μM	SANGER
J82	Growth Inhibition Assay		IC50=29.8013 μM	SANGER
MC116	Growth Inhibition Assay		IC50=30.0733 μM	SANGER
NCI-H69	Growth Inhibition Assay		IC50=30.6093 μM	SANGER
NB6	Growth Inhibition Assay		IC50=31.3629 μM	SANGER
CAL-120	Growth Inhibition Assay		IC50=32.4317 μM	SANGER
U-87-MG	Growth Inhibition Assay		IC50=33.0251 μM	SANGER
NCI-H1304	Growth Inhibition Assay		IC50=33.0354 μM	SANGER
YH-13	Growth Inhibition Assay		IC50=33.2535 μM	SANGER
RMG-I	Growth Inhibition Assay		IC50=33.4285 μM	SANGER
LU-65	Growth Inhibition Assay		IC50=34.1408 μM	SANGER
GB-1	Growth Inhibition Assay		IC50=35.0729 μM	SANGER
DU-4475	Growth Inhibition Assay		IC50=35.1553 μM	SANGER
SBC-5	Growth Inhibition Assay		IC50=36.5902 μM	SANGER
OE33	Growth Inhibition Assay		IC50=37.7577 μM	SANGER
C8166	Growth Inhibition Assay		IC50=38.5267 μM	SANGER
COLO-684	Growth Inhibition Assay		IC50=38.7428 μM	SANGER
NCI-H1155	Growth Inhibition Assay		IC50=39.0471 μM	SANGER
ATN-1	Growth Inhibition Assay		IC50=39.7792 μM	SANGER
KARPAS-299	Growth Inhibition Assay		IC50=39.839 μM	SANGER
KNS-81-FD	Growth Inhibition Assay		IC50=40.3604 μM	SANGER
NCI-H1563	Growth Inhibition Assay		IC50=41.5039 μM	SANGER
NB14	Growth Inhibition Assay		IC50=42.7263 μM	SANGER
COLO-800	Growth Inhibition Assay		IC50=42.8517 μM	SANGER
MS-1	Growth Inhibition Assay		IC50=43.0483 μM	SANGER
OVCAR-8	Growth Inhibition Assay		IC50=43.6809 μM	SANGER
SK-PN-DW	Growth Inhibition Assay		IC50=43.8776 μM	SANGER
G-402	Growth Inhibition Assay		IC50=43.9006 μM	SANGER
NCI-H2291	Growth Inhibition Assay		IC50=44.8017 μM	SANGER
PC-3	Growth Inhibition Assay		IC50=45.8023 μM	SANGER
NCI-H1581	Growth Inhibition Assay		IC50=45.9889 μM	SANGER
SW1116	Growth Inhibition Assay		IC50=47.0182 μM	SANGER
ZR-75-30	Growth Inhibition Assay		IC50=47.0239 μM	SANGER
OCI-AML2	Growth Inhibition Assay		IC50=47.0918 μM	SANGER
MDA-MB-231	Growth Inhibition Assay		IC50=47.6249 μM	SANGER
ES3	Growth Inhibition Assay		IC50=48.3529 μM	SANGER
NCI-H630	Growth Inhibition Assay		IC50=49.1742 μM	SANGER
OE19	Growth Inhibition Assay		IC50=49.2902 μM	SANGER
NCI-H1573	Growth Inhibition Assay		IC50=49.6861 μM	SANGER
EW-1	Growth Inhibition Assay		IC50=49.9084 μM	SANGER
K562	Cytotoxicity assay	72 hrs	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0043 μM.	26814890
HEK293	Function assay	1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0127 μM.	29941193
fibroblast cells	Antiproliferative assay		Antiproliferative activity against Src-transformed rat2 fibroblast cells, IC50 = 0.1 μM.	17181170
fibroblast cells	Function assay		Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA, IC50 = 0.1 μM.	17905586
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.128 μM.	30137981
HEK293	Function assay	1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.133 μM.	29941193
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.14 μM.	30137981
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.146 μM.	30137981
Ba/F3	Function assay		Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay, IC50 = 0.15 μM.	16970400
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.177 μM.	30137981
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.195 μM.	30137981
Ba/F3	Antiproliferative assay		Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 0.2 μM.	16970400
Ba/F3	Function assay		Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay, IC50 = 0.2 μM.	16970400
Ba/F3	Function assay	48 hrs	Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.204 μM.	30137981
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.243 μM.	30137981
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.278 μM.	30137981
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.356 μM.	30137981
fibroblast cells	Function assay		Inhibitory concentration against Abl transformed rat fibroblast cells, IC50 = 0.49 μM.	16161995
Ba/F3	Function assay	48 hrs	Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.642 μM.	30137981
Ba/F3	Antiproliferative assay		Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 1 μM.	16970400
HepG2	Antiproliferative assay	48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.15 μM.	18485715
HT29	Antiproliferative assay	48 hrs	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.17 μM.	18485715
BA/F3	Cytotoxicity assay	72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 3.2 μM.	26814890
HeLa	Function assay	4.5 hrs	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 3.85 μM.	29624387
HT29	Antiproliferative assay	48 hrs	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.87 μM.	18485715
HepG2	Antiproliferative assay	48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.91 μM.	18485715
HT29	Antiproliferative assay	48 hrs	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, TGI = 6.5 μM.	18485715
HepG2	Antiproliferative assay	48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, TGI = 7.66 μM.	18485715
Ba/F3	Cell death assay		Induction of cell death of murine BaF3 cells expressing NPM/ALK L256T mutant by trypan blue exclusion assay	16970400
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
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Informations chimiques, stockage et stabilité

Poids moléculaire	530.45	Formule	C₂₆H₂₉Cl₂N₅O₃	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	380843-75-4	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	SKI-606			Smiles	CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (188.51 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	1%DMSO 1 40%PEG300 2 5%Tween80 3 54%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	0.625mg/ml (1.18mM)	Taking the 1 mL working solution as an example, add 10 μL of 62.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 540 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (9.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	0.650mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	S6 kinase ERK STAT3 LCK Abl (Cell-free assay) 1 nM Src (Cell-free assay) 1.2 nM
In vitro	Le Bosutinib est sélectif pour Src par rapport aux kinases non-Src, avec une IC50 de 1,2 nM, et inhibe puissamment la prolifération cellulaire dépendante de Src avec une IC50 de 100 nM. Ce composé inhibe significativement la prolifération des lignées cellulaires leucémiques Bcr-Abl-positives KU812, K562 et MEG-01 mais pas Molt-4, HL-60, Ramos et d'autres lignées cellulaires leucémiques, avec des IC50 de 5 nM, 20 nM et 20 nM respectivement, plus puissamment que celle du STI-571. Similaire au STI-571, il présente une activité antiproliférative contre les fibroblastes transformés par Abl-MLV avec une IC50 de 90 nM. Ce produit chimique ablates la phosphorylation de la tyrosine de Bcr-Abl et STAT5 dans les cellules LMC et de v-Abl exprimé dans les fibroblastes à la concentration de ~50 nM, 10-25 nM et 200 nM respectivement, conduisant à l'inhibition de la signalisation en aval de Bcr-Abl de la phosphorylation de Lyn/Hck. Bien qu'incapable d'inhiber la prolifération et la survie des cellules cancéreuses du sein, il diminue significativement la motilité et l'invasion des cellules cancéreuses du sein avec une IC50 d'environ 250 nM, impliquant une augmentation de l'adhésion cellule-cellule et de la localisation membranaire de la β-caténine.
Essai kinase	Les essais kinases Src et Abl
Essai kinase	L'activité de la kinase Src est mesurée par ELISA. Src (3 unités/réaction), le tampon de réaction (50 mM Tris-HCl pH 7,5, 10 mM MgCl₂, 0,1 mM EGTA, 0,5 mM Na₃VO₄) et le peptide substrat cdc2 sont ajoutés à diverses concentrations de Bosutinib et incubés à 30 °C pendant 10 minutes. La réaction est démarrée par l'ajout d'ATP à une concentration finale de 100 μM, incubée à 30 °C pendant 1 heure et arrêtée par l'ajout d'EDTA. Les instructions du fabricant sont suivies pour les étapes ultérieures. L'essai de la kinase Abl est réalisé dans un format de détection DELFIA en phase solide à base d'europium. Le peptide biotinylé (2 μM) est lié à des plaques de microtitration revêtues de streptavidine pendant 1,5 heure dans 1 mg/mL d'ovalbumine dans du PBS. Les plaques sont lavées pendant 1 heure avec du PBS/0,1 % Tween 80, suivi d'un lavage au PBS. La réaction de la kinase est incubée pendant 1 heure à 30°C. La kinase Abl (10 unités) est mélangée avec 50 mM Tris-HCl (pH 7,5), 10 mM MgCl₂, 80 μM EGTA, 100 μM ATP, 0,5 mM Na₃VO₄, 1 % DMSO, 1 mM HEPES (pH 7,0), 200 μg/mL d'ovalbumine et diverses concentrations de ce composé. La réaction est arrêtée avec de l'EDTA à une concentration finale de 50 mM. La réaction est surveillée avec un anticorps anti-phosphotyrosine marqué à l'Europium et une solution d'amélioration DELFIA.
In vivo	Le Bosutinib (60 mg/kg/jour) est actif contre les xénogreffes de fibroblastes transformés par Src et les xénogreffes HT29 chez des souris nues avec des T/C de 18 % et 30 % respectivement. L'administration orale de ce composé pendant 5 jours supprime significativement la croissance tumorale K562 chez les souris de manière dose-dépendante, les grosses tumeurs étant éradiquées à une dose de 100 mg/kg et les souris étant exemptes de tumeurs à 150 mg/kg sans toxicité manifeste. Étant inactif contre les xénogreffes Colo205 chez les souris nues à 50 mg/kg deux fois par jour, l'administration de ce produit chimique à 75 mg/kg deux fois par jour est nécessaire contre les xénogreffes Colo205, et l'augmentation de la dose de ce composé n'apporte aucun bénéfice supplémentaire, contrairement à la capacité dose-dépendante significative contre les xénogreffes HT29.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/11689083/ [2] https://pubmed.ncbi.nlm.nih.gov/12543790/ [3] https://pubmed.ncbi.nlm.nih.gov/18483306/ [4] https://pubmed.ncbi.nlm.nih.gov/15958584/ [5] https://pubmed.ncbi.nlm.nih.gov/20445575/ [6] https://pubmed.ncbi.nlm.nih.gov/21206976/ [7] https://pubmed.ncbi.nlm.nih.gov/27903968/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	p-ABL / ABL p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3	28199182
Immunofluorescence	p-FAK / p-STAT3 / beta-catenin	18483306
Growth inhibition assay	IC50 Cell viability	27903968

Informations sur lessai clinique

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT05363488	Completed	Myeloid Leukemia	Pfizer	October 8 2021	--
NCT04258943	Active not recruiting	Philadelphia Chromosome Positive CML\|Accelerated Phase Chronic Myelogenous Leukemia\|Blastic Phase Chronic Myelogenous Leukemia\|Chronic Phase Chronic Myelogenous Leukemia	Children''s Oncology Group\|Erasmus Medical Center\|Dutch Childhood Oncology Group\|Innovative Therapies for Children with Cancer\|Pfizer	April 6 2020	Phase 1\|Phase 2
NCT03023319	Completed	Carcinoma Non-Small-Cell Lung\|Mesothelioma\|Bladder Cancer\|Ovarian Cancer\|Peritoneal Cancer\|Thymoma\|Thymus Cancer\|Uterine Cervical Cancer	Nagla Abdel Karim\|Augusta University	December 10 2019	Phase 1
NCT03888222	Completed	Dementia With Lewy Bodies	Georgetown University\|Alzheimer''s Association	April 23 2019	Phase 2
NCT03854903	Active not recruiting	Metastatic Breast Cancer\|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast\|Hormone Receptor Positive Breast Cancer	Georgetown University\|Pfizer	April 1 2019	Phase 1

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Foire aux questions

Question 1:
Can I give S1014 to mice by oral gavage? If so, how to dissolve it?

Réponse :
For oral gavage, it can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):