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Bms-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50 of 100 nM and 73 nM, respectively. It also showed moderate inhibitory activity against Mek, Fak and Lck, but almost no inhibitory activity against Akt1 and MAPK1/2.
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Source | Onco Targets Ther (2015). Figure 1. BMS-536924 |
| Method | cell viability assay | |
| Cell Lines | TMZ-resistant cells | |
| Concentrations | 400 nM | |
| Incubation Time | 24, 48, or 72 h | |
| Results | BMS-536924 also significantly reduced the viability of both TMZ-sensitive and -resistant lines, in a time-dependent manner |
| Cell Experiment | |
|---|---|
| Cell lines | TGBC-1TKB, TGBC-2TKB and TGBC-14TKB cell lines |
| Preparation method | In vitro cell growth. Four thousand cells were seeded into a 96-well plate and each was treated with several concentrations of BMS-536924. Cell growth was measured using WST-1 reagent, as described previously. |
| Concentrations | 0, 1, 5, 10μM |
| Incubation time | 0, 1, 2, 3, 4 days |
| Animal Experiment | |
|---|---|
| Animal models | TGBC-1TKB tumour xenograft in nude mice |
| Formulation | a mixture of polyethylene glycol 400 (PEG400 ⁄ water, 4:1 vol ⁄ vol) |
| Dosages | 70 mg ⁄ kg once daily for 2 weeks |
| Administration | oral gavage |
| Molecular Weight | 479.96 |
| Formula | C25H26ClN5O3 |
| CAS Number | 468740-43-4 |
| Solubility (25°C) | DMSO 66 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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