生物活性
OSI-930是Kit，KDR，Flt，CSF-1R，c-Raf和Lck的有效抑制剂，IC50分别为80 nM，9 nM，8 nM，15 nM，41 nM和22 nM。
Targets
| Target | Value |
| FLT1 | IC50: 8nM |
| KDR | IC50: 9nM |
| CSF-1R | IC50: 15nM |
| LCK | IC50: 22nM |
| C-Raf | IC50: 41nM |
| Kit | IC50: 80nM |
| FLT3 | IC50: 1.303μM |
| PDGFRα | IC50: 3.408μM |
| Abl | IC50: 4.738μM |
| PDGFRβ | IC50: 6.9μM |
| EGFR | IC50: >10μM |
| AuroraA | IC50: >10μM |
| Axl | IC50: >10μM |
| CDK2/CyclinA | IC50: >10μM |
| IKKβ | IC50: >10μM |
| MEK1 | IC50: >10μM |
| PDPK1 | IC50: >10μM |
| PKBβ | IC50: >10μM |
| Tie-2 | IC50: >10μM |
化学数据
| 目录号 | A10679 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 443.4 |
| Formula | C22H16F3N3O2S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 728033-96-3 |
| Synonyms | OSI930 |
| SMILES | C1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(F)(F)F |
溶解度
| In vitro (25°C) | DMSO | 85 mg/mL (191.68 mM) |
| Water | Insoluble |
| Ethanol | 3 mg/mL |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 4 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 22.55 mL | 112.76 mL | 225.53 mL |
| 0.5 mM | 4.51 mL | 22.55 mL | 45.11 mL |
| 1 mM | 2.26 mL | 11.28 mL | 22.55 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.51 mL |
*The above data is based on the productmolecular weight 443.4 . 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.
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