Bioactivity | 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[1][2]. | |||||||||
Invitro | BMS-536924 inhibits FAK and Lck with IC50s of 150 nM and 341 nM, respectively[1]. BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation[2]. BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC50 of 0.48 μM[2]. BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini[2]. BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block[2]. 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[2]. Cell Proliferation Assay[2] Cell Line: | |||||||||
Name | BMS-536924 | |||||||||
CAS | 468740-43-4 | |||||||||
Formula | C25H26ClN5O3 | |||||||||
Molar Mass | 479.96 | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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