Home PI3K/Akt/mTOR PI3K inhibiteur Buparlisib (BKM120)

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Buparlisib (BKM120) Inhibiteur de PI3K

Réf. CatalogueS2247

Buparlisib (BKM120, NVP-BKM120) est un inhibiteur sélectif de PI3K de p110α/β/δ/γ avec une IC50 de 52 nM/166 nM/116 nM/262 nM dans des tests sans cellules, respectivement. Puissance réduite contre VPS34, mTOR, DNAPK, avec peu d'activité sur PI4Kβ. Buparlisib induit l'apoptose. Phase 2.
Buparlisib (BKM120) PI3K inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 410.39

Aller à

Contrôle Qualité

Lot : Pureté : 99.94%
99.94

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires Type dessai Concentration Temps dincubation Formulation Description de lactivité PMID
glioma cell lines Growth Inhibition Assay 72h IC50=1-2μM 22065080
U87 Apoptosis Assay 2μM 72h induces cell apoptosis and cleaved PARP and caspase-3 22065080
SNU-601 Growth Inhibition Assay 72h DMSO IC50=0.816±0.063μM 22159814
SNU-1 Growth Inhibition Assay 72h DMSO IC50=1.082±0.028μM 22159814
SNU-668 Growth Inhibition Assay 72h DMSO IC50=1.579±0.074μM 22159814
AGS Growth Inhibition Assay 72h DMSO IC50=1.714±0.117μM 22159814
SNU-216 Growth Inhibition Assay 72h DMSO IC50=2.692±0.082μM 22159814
SNU-5 Growth Inhibition Assay 72h DMSO IC50=1.351±0.091μM 22159814
SNU-638 Growth Inhibition Assay 72h DMSO IC50=2.282±0.053μM 22159814
SNU-16 Growth Inhibition Assay 72h DMSO IC50=1.573±0.001μM 22159814
SNU-484 Growth Inhibition Assay 72h DMSO IC50=1.728±0.045μM 22159814
SNU-620 Growth Inhibition Assay 72h DMSO IC50=2.939±0.001μM 22159814
SNU-719 Growth Inhibition Assay 72h DMSO IC50=3.037±0.032μM 22159814
MM cell lines Growth Inhibition Assay 10μM 24h DMSO IC50 varies among different cell lines in time and dose dependence 22207485
ARP-1 Apoptosis Assay 10μM 24h DMSO induces MM cell apoptosis through caspase activation 22207485
colon cancer cell lines Growth Inhibition Assay 0-10μM 72h DMSO IC50=1μM 22543857
gastric cancer cell lines Growth Inhibition Assay 0-10μM 72h DMSO IC50=2-5μM 22543857
HCT-116/HT-29/MKN-45 Apoptosis Assay 2μM 48h shift in G2 phase 22543857
HT-29 and HCT-116 Caspase assay 5μM 24h induces caspase activity 22543857
PIK3CA-mutant MCF7 Growth Inhibition Assay GI50=160±91nM，LD50=980±273nM 72h GI50=160±91nM，LD50=980±273nM 22653967
PIK3CA-mutant MCF7 Kinase Assay IC50=114±3nM 72h IC50=114±3nM in reducing Akt phosphorylation levels 22653967
MCF7-myr-Akt Growth Inhibition Assay GI50=299±68nM，LD50＞10,000nM 72h GI50=299±68nM，LD50＞10,000nM 22653967
Y1 cell line Growth Inhibition Assay 0.1μM/1μM 24h DMSO inhibits 60％ cell viability in Myc-Sctr-transfected cells 22692904
human NSCLC Growth Inhibition Assay 0.5-2μM 72h IC50=1μM 22781393
human NSCLC Kinase Assay 1μM 24h inhibits the Akt/mTOR signaling pathway at 3h after treatment 22781393
JVM2 Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.9μM 23238639
EHEB Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.7μM 23238639
MEC2 Cytotoxicity assay 0.2-20μM 72h DMSO IC50=0.7μM 23238639
primary B-CLL lymphocytes Apoptosis Assay IC50 for each primary cell line 24h DMSO IC50＜3μM for all patients 23238639
primary B-CLL lymphocytes Kinase Assay IC50 for each primary cell line 24h inhibits p70S6K & 4E-BP1 expression 23238639
SK-HEP1 Growth Inhibition Assay 1-20μM 72h DMSO IC50＜1μM 23479136
786-0 Growth Inhibition Assay 1-20μM 72h DMSO IC50＜1μM 23479136
human HCC cell lines Cell viability assay 0.005-1μM 48h IC50=1μM 23489999
Huh7 Kinase Assay 1μM 48h significantly reduces phosphorylation of Akt 23489999
human NSCLC cell lines Apoptosis Assay 0.125-4μM 24h DMSO IC50s ranges from 0.4-2μM 23562472
Primary CLL cells Apoptosis Assay 1-10μM 48h induces apoptosis in CLL cells independent of prognostic markers 23850807
Primary CLL cells Kinase Assay 2μM 30min decreased PI3K activity 23850807
Primary CLL cells Cytotoxic Assay 2μM 24h induces cell cytotoxicity 23850807
LC-1/SQSF Function Assay 3μM 24h DMSO decrease NRF2 protein level 23980093
BCR-ABL Growth Inhibition Assay 0.25-10μM 4d significantly inhibit cell proliferation 24244612
T-ALL Apoptosis Assay between 1.4 and 5.3 mM at 24h and 0.9 and 5.5 mM at 48h in different cell line 24 or 48h DMSO affects the PI3K pathway in T-ALL cell lines 24310736
H1975 Growth Inhibition Assay 0.3-9.6μM 72h DMSO IC50=1.385μM 24337846
H1975 Apoptosis Assay 2μM 24h DMSO increases apoptosis rate significantly 24337846
BON Growth Inhibition Assay 1-5μM 72h decreases cell proliferation 24443523
BON Apoptosis Assay 1-5μM 24h increases apoptosis 24443523
GBM Apoptosis Assay 2μM 48h DMSO induced higher levels of apoptosis, and decreased cell viability 24500492
FaDu Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
EMT6 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
HCT116 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
U87 Function Assay 5 μM 24 h DMSO Reduces oxygen consumption 24631147
Saos-2 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
MG-63 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
SJSA-1 Function Assay 50 μM 48 h Inhibits cell invasion 24727660
Saos-2 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
MG-63 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
SJSA-1 Function Assay 50 μM 48 h Inhibits matrix metalloproteinase-2 expression 24727660
Saos-2 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
MG-63 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
SJSA-1 Growth Inhibition Assay 50 μM 48 h Inhibits cell viability 24727660
LN18 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LN229 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LNZ308 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
T98G Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
U87 Growth Inhibition Assay 20 μM 72 h DMSO IC50<5 μM 24741074
LN18 Function Assay 5 μM 24 h DMSO Inhibits phosphorylation of AKT 24741074
LNZ308 Function Assay 5 μM 24 h DMSO Inhibits phosphorylation of AKT 24741074
MDA-MB-175 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-134 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1500 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
EFM-19 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
ZR-75-30 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-361 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
T-47D Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
SK-BR-3 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
UACC-732 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-474 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC202 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MCF7 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-415 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-453 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
ZR-75-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC38 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1419 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
UACC-812 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1187 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
KPL-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
SUM-225 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
EFM-192A Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
JIMT-1 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1143 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC2218 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-468 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-20 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MDA-MB-435 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
BT-549 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1806 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
HCC1937 Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
Hs578T Growth Inhibition Assay 1 μM 5 d DMSO IC50<1 μM 24879796
MCF7 Cytotoxic Assay 72 h DMSO Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 μM 24900266
DU145 Cytotoxic Assay 72 h DMSO Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 μM 24900266
A2780 Cytotoxic Assay 72 h DMSO Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 μM 24900266
U87MG Cytotoxic Assay 72 h DMSO Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 μM 24900266
A2780 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 μM 24900266
DU145 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation with EC50 of 0.073 μM 24900266
A2780 Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells with EC50 of 0.074 μM 24900266
MCF7 Function Assay 1 h DMSO Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 μM 24900266
U87MG Function Assay 1 h DMSO Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells with EC50 of 0.13 μM 24900266
A2780 Growth Inhibition Assay 72 h DMSO EC50=0.52 μM 24900266
Huh7 Function Assay 1 μM 1 h DMSO Inhibits phosphorylation of AKT at Ser474 25004403
BNL Function Assay 1 μM 1 h DMSO Inhibits phosphorylation of S6 25004403
BON-1 Growth Inhibition Assay 500 nM 10 d DMSO Inhibits cell growth 25026292
BON-1 Function Assay 500 nM 4 h DMSO Inhibits phosphorylation of AKT at Thr308 and Ser473 25026292
QGP-1 Function Assay 500 nM 4 h DMSO Inhibits phosphorylation of AKT at Thr308 and Ser473 25026292
HCT-15 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation 25152245
HCT-116 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation 25152245
NCI-H460 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation 25152245
SKOV-3 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation 25152245
BSY-1 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation 25152245
MKN-1 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation 25152245
NCI-H522 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
OVCAR-3 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
HBC-5 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
RXF-631L Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
MKN-45 Apotosis Assay 10 μM 48 h DMSO Induces apoptosis 25152245
LNCaP Function Assay 1 μM Suppresses p-AKT levels 25360799
LNCaP95 Function Assay 1 μM Suppresses p-AKT levels 25360799
A549 Function Assay 500 nM 48 h DMSO Inhibits Akt activation 25937299
A549 Growth Inhibition Assay 1 μM 72 h DMSO Inhibits cell growth 25937299
H522 Growth Inhibition Assay 1 μM 72 h DMSO Inhibits cell growth 25937299
SKMES-1 Cytotoxic Assay 1 μM 72 h Induces cell death 26013318
H596 Function Assay 1 μM Impairs cell migration 26013318
HCC2450 Function Assay 1 μM Impairs cell invasion 26013318
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.48 μM. 25765909
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 1 μM. 25765909
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.64 μM. 25765909
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 2.07 μM. 25765909
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50 = 4.34 μM. 25765909
HCT116 Function assay 10 uM 1 hr Inhibition of PI3K/Akt in human HCT116 cells assessed as Akt phosphorylation at 10 uM after 1 hr by Western blotting analysis 25765909
A2058 melanoma Cell cycle assay 5 uM 24 hrs Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at SubG1 phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
A2058 melanoma Cell cycle assay 5 uM 24 hrs Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
SKOV3 Cell cycle assay 2 uM 24 hrs Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
SKOV3 Cell cycle assay 2 uM 24 hrs Cell cycle arrest in human SKOV3 cells assessed as accumulation at SubG1 phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis 28829592
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.88 μM. 29107429
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 5.34 μM. 29107429
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.92 μM. 29107429
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 11.05 μM. 29107429
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
insect Function assay Inhibition of recombinant human His-tagged p85alpha/p110alpha E545K mutant expressed in insect cells, IC50 = 0.011 μM. 30034607
insect Function assay Inhibition of recombinant human His-tagged p85alpha/p110alpha E542K mutant expressed in insect cells, IC50 = 0.029 μM. 30034607
Sf21 Function assay 1 hr Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polar, IC50 = 0.125 μM. 30034607
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay, IC50 = 0.206 μM. 30034607
Sf21 Function assay 1 hr Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polari, IC50 = 0.234 μM. 30034607
T47D Antiproliferative assay 72 hrs Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay, IC50 = 0.286 μM. 30034607
PC3 Function assay 2 hrs Inhibition of PI3K in human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 measured after 2 hrs by fluorescence assay, IC50 = 0.365 μM. 30034607
HT-29 Cell cycle assay 0.111 to 3 uM 24 hrs Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 0.111 to 3 uM after 24 hrs by propidium iodide staining based flow cytometry 30034607
A2058 Function assay 1 hr Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis, IC50 = 0.416 μM. 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis, IC50 = 0.553 μM. 30359003
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Informations chimiques, stockage et stabilité

Poids moléculaire 410.39 Formule

C18H21F3N6O2

 Stockage (À compter de la date de réception)
N° CAS 944396-07-0 Télécharger le SDF Stockage des solutions mères

Synonymes NVP-BKM120 Smiles C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

Solubilité

In vitro
Lot:

DMSO : 82 mg/mL (199.8 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 25 mg/mL

Water : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

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)

mg/kg g μL

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
p110α
(Cell-free assay)
52 nM
p110δ
(Cell-free assay)
116 nM
p110β
(Cell-free assay)
166 nM
p110γ
(Cell-free assay)
262 nM
Vps34
(Cell-free assay)
2.4 μM
mTOR
(Cell-free assay)
4.6 μM
In vitro
Le Buparlisib (BKM120) n'est pas sensible aux PI3K de classe III et IV ou à la PI4K. Il montre une grande activité antiproliférative sur les lignées cellulaires dérégulées par PI3K, y compris A2780, U87MG, MCF7 et DU145, avec une GI50 de 0,1-0,7 nM. Ce composé induit l'apoptose des cellules de myélome multiple (ARP1, ARK, MM.1S, MM1.R et U266), ce qui entraîne une augmentation des cellules en phase G1 et une diminution des cellules en phase S. Il a également induit l'apoptose des cellules primaires de MM CD138+ et a une cytotoxicité significativement plus faible envers les cellules stromales CD138−. Son exposition pourrait entraîner une régulation positive de BimS et une régulation négative de XIAP. Le BKM120 démontre une activité antiproliférative dans les lignées cellulaires de cancer gastrique humain en diminuant la signalisation en aval de mTOR. Il pourrait augmenter soit p-ERK, soit p-STAT3 dans les cellules de cancer gastrique mutantes KRAS. La combinaison avec un blocage de STAT3 montre un synergisme dans les cellules hébergeant un KRAS muté en induisant l'apoptose, mais pas dans les cellules de type sauvage KRAS. Une étude récente montre qu'il présente des formes différentielles de mort cellulaire en fonction du statut p53 des cellules, les cellules de type sauvage p53 subissant une mort cellulaire apoptotique et les cellules mutantes/délétées p53 ayant une mort cellulaire par catastrophe mitotique. Il médie la catastrophe mitotique principalement par la kinase Aurora B.
Essai kinase
Essai biochimique de PI3K (essai de déplétion d'ATP)
Le Buparlisib (BKM120) est dissous dans du DMSO et directement distribué dans une plaque noire de 384 puits à raison de 1,25 µL par puits. Pour démarrer la réaction, 25 µL de 10 nM de PI3 kinase et 5 µg/mL de 1-α-phosphatidylinositol (PI) dans le tampon d'essai (10 mM Tris pH 7,5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT et 0,05% CHAPS) sont ajoutés à chaque puits, suivis de 25 µL de 2 µM d'ATP dans le tampon d'essai. La réaction est effectuée jusqu'à ce qu'environ 50% de l'ATP soit épuisé, puis arrêtée par l'ajout de 25 µL de solution KinaseGlo. La réaction arrêtée est incubée pendant 5 minutes et l'ATP restant est ensuite détecté par luminescence.
In vivo
Le Buparlisib (BKM120) inhibe complètement pAktser473 dans les xénogreffes tumorales A2780 à des doses de 30, 60 ou 100 mg/kg, respectivement, et montre également une activité antitumorale contre le modèle de gliome U87MG à des doses de 30 et 60 mg/kg. Le traitement par ce composé entraîne une réduction significative du volume tumoral et du niveau de chaîne kappa humaine circulante à 5 μM/kg/jour−1 dans le modèle de souris ARP1 SCID, avec une survie prolongée.
Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/22065080/

Applications

Méthodes Biomarqueurs Images PMID
Western blot p-MET / MET p-STAT3 / STAT3 / p-ERK / ERK / p-S6 p-ERK / ERK / LC3 Nuclear NF-κB p65 / NF-κB p65 p-FOXO3a (S253) / FOXO3a p-AKT (T308) / p-AKT (S473) / AKT
S2247-WB6
29928341
Immunofluorescence FOXO3a
S2247-IF1
28036259
Growth inhibition assay Cell viability
S2247-viability1
26673665

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
NCT04338399 Active not recruiting
Head and Neck Cancer
Adlai Nortye Biopharma Co. Ltd.
 December 12 2020 Phase 3
NCT02614508 Terminated
Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma
Emory University|Novartis
 January 2016 Phase 1
NCT01613677 Withdrawn
Treatment for Metastatic or Locally Advanced Cervical Cancer
Novartis Pharmaceuticals|Novartis
 November 2015 Phase 2

Support technique

Instructions de manipulation

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