生物活性
PHA665752是c-Met/HGF/SF信号传导的小分子抑制剂。
Targets
| Target | Value |
| c-Met | IC50: 9nM |
| RON | IC50: 68nM |
| Flk1 | IC50: 200nM |
| c-Abl | IC50: 1.4μM |
| FGFR1 | IC50: 3μM |
| EGFR | IC50: 3.8μM |
| c-Src | IC50: 6μM |
| IGF-1R | IC50: >10μM |
| PDGFR | IC50: >10μM |
| AuroraA2 | IC50: >10μM |
| PKA | IC50: >10μM |
| PKBα | IC50: >10μM |
| CDK2 | IC50: >10μM |
| p38α | IC50: >10μM |
| MK2 | IC50: >10μM |
| MK3 | IC50: >10μM |
化学数据
| 目录号 | A10713 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 641.6 |
| Formula | C32H34Cl2N4O4S |
| 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. | 477575-56-7 |
| Synonyms | PHA665752 |
| SMILES | CC1=C(NC(=C1C(=O)N2CCC[C@@H]2CN3CCCC3)C)/C=C\4/C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O |
溶解度
| In vitro (25°C) | DMSO | 124 mg/mL (193.26 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+castor oil | 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 | 15.59 mL | 77.93 mL | 155.86 mL |
| 0.5 mM | 3.12 mL | 15.59 mL | 31.17 mL |
| 1 mM | 1.56 mL | 7.79 mL | 15.59 mL |
| 5 mM | 0.31 mL | 1.56 mL | 3.12 mL |
*The above data is based on the productmolecular weight 641.6 . 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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