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$0.00 - Qiao Zhou, .et al. BMS-536924, an ATP-competitive IGF-1R/IR inhibitor, decreases viability and migration of temozolomide-resistant glioma cells in vitro and suppresses tumor growth in vivo, Onco Targets Ther., 2015, 8: 689-697 PMID: 25897243
Biological Activity
BMS-536924 is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype.
Targets
| Target | Value |
|---|---|
| Insulin Receptor | IC50: 73nM |
| IGF-1R | IC50: 100nM |
| FAK | IC50: 150nM |
| MEK | IC50: 182nM |
| LCK | IC50: 341nM |
| CDK2/CyclinE | IC50: >1μM |
| VEGFR2 | IC50: 1.4μM |
| EGF | IC50: 1.6μM |
| Met | IC50: 4.87μM |
| MAPK2 | IC50: ~5μM |
| MAPK1 | IC50: >5μM |
| Akt1 | IC50: >5μM |
| PDGFR | IC50: >5μM |
| HER2 | IC50: 17.1μM |
| In vitro (25°C) | DMSO | 92 mg/mL (191.68 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 20.83 mL | 104.17 mL | 208.33 mL |
| 0.5 mM | 4.17 mL | 20.83 mL | 41.67 mL |
| 1 mM | 2.08 mL | 10.42 mL | 20.83 mL |
| 5 mM | 0.42 mL | 2.08 mL | 4.17 mL |
*The above data is based on the productmolecular weight 480.0 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11054 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 468740-43-4 |
| Formula | C25H26ClN5O3 |
| M. Wt | 480.0 |
| Purity | >98% |
| Synonyms | BMS536924 |
| SMILES | CC1=CC(=CC2=C1N/C(=C/3\C(=CC=NC3=O)NC[[email protected]](C4=CC(=CC=C4)Cl)O)/N2)N5CCOCC5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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