BMS-536924

SKU: orb1940999

Description

BMS-536924 is a potent small molecule inhibitor of IGF-IR, which shows antitumor activity in multiple tumor models, including sarcoma.(In Vitro):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.(In Vivo):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.

Key Properties

• CAS Number: 468740-43-4
• MW: 479.96
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₆ClN₅O₃
• SMILES: CC1=C2N=C(NC2=CC(=C1)N1CCOCC1)C1=C(NC[C@@H](O)C2=CC=CC(Cl)=C2)C=CNC1=O
• Target: FAK| IGF-1R| Insulin Receptor| MEK| Lck
• Solubility: DMSO : 50 mg/mL. 104.18 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS536924 | BMS-536924 | BMS 536924

Quick Database Links

Gene Symbol

FAK| IGF-1R| Insulin Receptor| MEK| Lck