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Dabrafenib (GSK2118436) inhibiteur de BRAF

Name: Dabrafenib (GSK2118436)
Brand: Selleck Chemicals
SKU: S2807
Rating: 5 (319 reviews)

Réf. CatalogueS2807

Dabrafenib est un inhibiteur spécifique de la BRAF^V600E mutante avec une IC50 de 0,7 nM dans des essais acellulaires, avec une puissance 7 et 9 fois inférieure contre B-Raf(wt) et c-Raf, respectivement.

Dabrafenib (GSK2118436) Raf inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 519.56

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Contrôle Qualité

Lot : Pureté : 99.99%

99.99

Cibles apparentées	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Autre Raf Inhibiteurs	LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265)

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
	Kinase Assay				Inhibition of N-terminal His tagged B-Raf V600E mutant expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay with IC50 of 0.0007 μM	24900673
SK-MEL-28	Kinase Assay		1 h		Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM	24900673
HepG2	Kinase Assay				Inhibition of B-Raf V600E mutant in human HepG2 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM	24900673
COLO205	Growth Inhibition Assay				Inhibition of human COLO205 cell proliferation with IC50 of 0.007 μM	24900673
HepG2	Function Assay		45 min	DMSO	Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis with IC50 of 3.7 μM	24900673
HFF	Growth Inhibition Assay	10 μM	72 h	DMSO	Inhibition of proliferation of human HFF cells harboring wild type B-Raf with IC50 of 3 μM	24900673
SK-MEL-28	Growth Inhibition Assay	10 μM	72 h	DMSO	Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation with IC50 of 0.043 μM	23844038
A375P-F11	Growth Inhibition Assay	10 μM	72 h	DMSO	Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation with IC50 of 0.071 μM	23844038
MALME-3M	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1 nM	23844038
UACC-62	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1 nM	23844038
C32TG	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1 nM	23844038
SK-MEL-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=2 nM	23844038
M14	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=2 nM	23844038
SK-MEL-28	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=3 nM	23844038
A375	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=4 nM	23844038
DU-4475	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=5 nM	23844038
UACC-257	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=6 nM	23844038
Colo 205	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=7 nM	23844038
SK-MEL-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=7 nM	23844038
SH-4	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=8 nM	23844038
A101D	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=9 nM	23844038
ES-2	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=53 nM	23844038
HT-29	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=66 nM	23844038
SW1417	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=158 nM	23844038
SW872	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=377 nM	23844038
RKO	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=2.522 μM	23844038
A673	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
GCT	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
WM-115	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=5 nM	23844038
YUMAC	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=5 nM	23844038
OV-90	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=29 nM	23844038
NCI-H508	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MDA-MB-231	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW756	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW-837	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
UMUC-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
LS-174T	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A549	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SHP-77	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW480	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
DLD-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HCT-116	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H747	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
T-84	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H460	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Calu-6	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HCC-2998	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
LS1034	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CHP-212	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-N-AS	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
BFTC-905	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HuT78	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=52 nM	23844038
RPMI-8226	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=263 nM	23844038
BC-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=277 nM	23844038
ACHN	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=294 nM	23844038
JRT3-T35	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=295 nM	23844038
SK-MES-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=329 nM	23844038
CESS	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=497 nM	23844038
H4	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=619 nM	23844038
BC-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=704 nM	23844038
DB	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=873 nM	23844038
RPMI-6666	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=928 nM	23844038
MC/CAR	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1.002 μM	23844038
SNU-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1.501 μM	23844038
CEM/C1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1.773 μM	23844038
GDM-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=1.997 μM	23844038
HT-1080	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=2.004 μM	23844038
HL-60	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=2.178 μM	23844038
C3A	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=5.414 μM	23844038
MES-SA	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=6.989 μM	23844038
22Rv1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
647-V	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
786-O	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A172	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A204	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A427	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A431	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A2780	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
ARH-77	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Be(2)C	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
BT-20	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
BxPc3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
C-4 I	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
C33A	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CAL-27	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CAL-62	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Calu-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CaOV3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CGTHW1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CHL-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Colo320DM	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Colo704	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
COR-L23	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
CRO-AP2	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Daudi	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
DOTC 24510	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
DU-145	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
EB-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
EFM-19	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
EKVX	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
FaDu	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
G401	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HCC-70	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HCC-1954	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Hela	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Hep3B	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HMCB	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HN5	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HOS	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HPAF-II	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Hs746.T	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HT	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HT-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
HuNS-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
IGROV1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
J82	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
JM1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Kato III	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
KHOS-240S	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
KM-12	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
KPL-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
KYSE-30	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
LNCaP	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MCF-7	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MC-IXC	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MDA-MB-175 VII	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MDA-MB-468	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
MiaPaCa	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Molt-4	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-ADR/RES	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H69	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H82	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-N87	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H146	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H157	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H187	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H209	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H226	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H292	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H322	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H358	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H520	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H526	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H630	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H661	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H716	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H1563	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H1792	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H2030	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H2052	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H2122	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
NCI-H2228	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OE-19	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OE-21	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OE-33	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OVCAR-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OVCAR-4	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
OVCAR-5	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
P3HR-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
PC-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
Raji	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
RD	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
RD-ES	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
RL	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SaOS2	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCC-9	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCC-12	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCC-13	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCC-15	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCC-25	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SCLC-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SF-268	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SF-295	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SJRH30	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-BR-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-LMS-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-N-DZ	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-N-F1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SKOV-3	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SK-UT-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SN12C	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SNB-19	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SNU-5	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SNU-16	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SNU-398	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SNU-449	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SR	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
ST486	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW579	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW684	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW-780	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW900	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW1088	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW1463	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
SW1990	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
T47D	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
TE381.T	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
TK-10	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
U2OS	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
U251	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
UACC-812	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
YAPC	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
ZR-75-1	Growth Inhibition Assay	10 μM	72 h	DMSO	IC50=10 μM	23844038
A375	Function assay	1.2 μM	4 h	DMSO	Inhibition of phosphorylation of MEK, ERK, and S6P	22389471
YUSIT1	Function assay			DMSO	reduced sensitivity with IC50 > 0.5 μM	22389471
MeWo	Growth inhibition assay			DMSO	IC50 = 987 nM	26018524
WiDr	Growth inhibition assay			DMSO	IC50 = 76 nM	26018524
Colo-205	Function assay	1 μM	4 d	DMSO	Induced a highly comparable compaction phenotype	25381152
RBW-1	Function assay	1 μM		DMSO	No reduction of Mek 1/2 phosphorylation	24885690
RBO-1	Function assay	1 μM		DMSO	Inhibition of Mek 1/2 phosphorylation	24885690
RBO-2	Function assay	1 μM		DMSO	Inhibition of Mek 1/2 phosphorylation	24885690
RBOW	Function assay	1 μM		DMSO	Inhibition of Mek 1/2 phosphorylation	24885690
M257	Growth Inhibition Assay	100 nM	72 h		Does not inhibit proliferation of M257 cell harbouring wild type BRAF	23317446
LCP	Growth Inhibition Assay	100 nM	72 h		Inhibition of proliferation of LCP cell harbouring BRAF V600R mutantation	23317446
WM266	Growth Inhibition Assay	100 nM	72 h		Inhibition of proliferation of WM266 cell harbouring BRAF V601D mutantation	23317446
M257	Growth Inhibition Assay	100 nM	72 h		Does not inhibit ERK1-2 phosphorylation in M257 cell harbouring wild type BRAF	23317446
LCP	Growth Inhibition Assay	100 nM	72 h		Inhibit ERK1-2 phosphorylation in LCP cell harbouring BRAF V600R mutantation	23317446
WM266	Growth Inhibition Assay	100 nM	72 h		Inhibit ERK1-2 phosphorylation in WM266 cell harbouring BRAF V600D mutantation	23317446
A375	BRAF competitive binding assay		15 min		IC50 = 0.006 μM	25965804
A375	Function assay		72 h		IC50 = 0.011 μM	25965804
A375	ARAF competitive binding assay		15 min		IC50 = 0.026 μM	25965804
A375	CRAF competitive binding assay		15 min		IC50 = 0.15 μM	25965804
HCT116	Function assay				IC50 = 5.88 μM	25965804
A375	Function assay		1 h		IC50 = 0.001 μM	27085672
MIAPaCa2	Function assay		1 h		EC50 = 0.529 μM	27085672
A375	Function assay				IC50 = 0.004 μM	29461827
SK-MEL-28	Cytotoxicity assay		72 h		IC50 = 0.043 μM	29461827
Sf9	Function assay		60 min		IC50 = 0.009 μM	27774137
SK-MEL-28	Growth inhibition assay		48 h		Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant measured after 48 hrs resazurin assay	27774137
SK-MEL-28	Growth inhibition assay		48 h		Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant preincubated for 1 hr followed by irradiation of 1.13 kW/m2 UV-light for 5 mins measured after 48 hrs resazurin assay	27774137
SK-MEL-28	Cytotoxicity assay		48 h		Cytostatic activity in human SK-MEL-28 cells harboring BRAF V600E mutant at 1 and 30 uM measured after 48 hrs resazurin assay	27774137
DAOY	Primary screen assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
NB1643	Primary screen assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
SK-N-MC	Primary screen 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	519.56	Formule	C₂₃H₂₀F₃N₅O₂S₂	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	1195765-45-7	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	GSK2118436, GSK2118436A			Smiles	CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (192.47 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.
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%PEG 300 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 (9.62mM)	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; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL 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.
Clear solution	2%DMSO 1 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	3.000mg/ml (5.77mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	2% DMSO 1 45% PEG300 2 2%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.	3.000mg/ml (5.77mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 450 μL PEG300, mix evenly to clarify it; add 20 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 510 μL 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.
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.	6.000mg/ml (11.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 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.

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	B-Raf (V600E) (Cell-free assay) 0.7 nM B-Raf (Cell-free assay) 5.2 nM C-Raf (Cell-free assay) 6.3 nM
In vitro	Le Dabrafenib est sélectif pour la kinase Raf, avec une sélectivité 400 fois supérieure pour B-Raf par rapport à 91 % des autres kinases testées. Ce composé inhibe la kinase B-Raf^V600E, entraînant une diminution de la phosphorylation d'ERK et une inhibition de la prolifération cellulaire par un arrêt initial en phase G1 du cycle cellulaire dans les cellules cancéreuses qui codent spécifiquement la mutation pour B-Raf^V600E.
In vivo	Le Dabrafenib (administré par voie orale) inhibe la croissance des xénogreffes tumorales humaines de mélanome mutant B-RafV600E (A375P) et de cancer du côlon (Colo205), qui se développent par voie sous-cutanée chez des souris immunodéprimées.
Références	[1] https://www.researchgate.net/publication/269940032_Abstract_B88_A_selective_Raf_kinase_inhibitor_induces_cell_death_and_tumor_regression_of_human_cancer_cell_lines_encoding_B-RafV600E_mutation [2] https://pubmed.ncbi.nlm.nih.gov/22389471/ [3] https://pubmed.ncbi.nlm.nih.gov/24900673/ [4] https://pubmed.ncbi.nlm.nih.gov/34296750/

Applications

Méthodes	Biomarqueurs	Images	PMID
Western blot	pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin		31158244
Growth inhibition assay	IC50		24735930

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
NCT06079333	Recruiting	Anaplastic Thyroid Cancer	Leiden University Medical Center\|Novartis	January 1 2023	Phase 2
NCT06337617	Completed	BRAF V600 Mutation Positive Melanoma	Novartis Pharmaceuticals\|Novartis	May 10 2022	--
NCT04961619	Recruiting	Melanoma	Novartis Pharmaceuticals\|Novartis	December 1 2021	--
NCT04547946	Completed	Malignant Melanoma	Novartis Pharmaceuticals\|Novartis	October 15 2021	--
NCT05171374	Recruiting	Melanoma Stage III\|Melanoma Stage IV\|Melanoma	MelanomaPRO Russia\|Novartis	September 30 2021	--

Support technique

Instructions de manipulation

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