BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.
IC50&Target
IC50: 100 nM (IGF-1R) and 73 nM (IR)
体外研究
BMS-536924 inhibits FAK and Lck with IC50s of 150 nM and 341 nM, respectively.
BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation.
BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC50 of 0.48 μM.
BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini.
BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block.
BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation.
Cell Proliferation Assay
Cell Line:
pBabe-MCF10A and CD8-IGF-IR-MCF10A acini
Concentration:
1 μM
Incubation Time:
Every four days for 12 days
Result:
Blocked acinar proliferation.
Cell Viability Assay
Cell Line:
CD8-IGF-IR-MCF10A cells
Concentration:
0.01, 0.1, 1 μM
Incubation Time:
24 hours
Result:
Has an IC50 of 0.48 μM.
Apoptosis Analysis
Cell Line:
CD8-IGF-IR-MCF10A acini
Concentration:
1 μM
Incubation Time:
For 4 days
Result:
Resulted in a dramatic induction of apoptosis.
Cell Cycle Analysis
Cell Line:
CD8-IGF-IR-MCF10A cells and pBabe-MCF10A control cells
Concentration:
0.1, 0.5, 1 μM
Incubation Time:
For 24 hours
Result:
Decreased in S-phase cells and caused a G0/G1 block.
Western Blot Analysis
Cell Line:
CD8-IGF-IR-MCF10A cells
Concentration:
1 μM
Incubation Time:
10 min, 1, 8, 24, 48 hours
Result:
Caused maximal inhibition of phosphorylated IGF-IR at 10 min and retained its ability to inhibit IGF-IR phosphorylation for up to 48 hours.
体内研究
BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks.
Animal Model:
Athymic nude mice with CD8-IGF-IRMCF10A cells
Dosage:
100 mg/kg
Administration:
Gavage; daily; for 35 days
Result:
Caused an average reduction of 76% tumor volume after 2 weeks.
分子式
C25H26N5O3Cl
分子量
479.96
CAS号
468740-43-4
运输条件
Room temperature in continental US; may vary elsewhere.