生物活性
AMG-458是一种有效的c-Met抑制剂，IC50值为60nM，对VEGFR2具有选择性。
Targets
| Target | Value |
| c-Met(H1094R) | ki: 0.5nM |
| c-Met(V1092I) | ki: 1.1nM |
| c-Met(Human) | ki: 1.2nM |
| c-Met(Mouse) | ki: 2.0nM |
| c-Met(D1228H) | ki: 2.2nM |
| c-Met(M1250T) | ki: 4.1nM |
| c-Met(Y1230H) | ki: 4.5nM |
| VEGFR2 | ki: 4.1μM |
化学数据
| 目录号 | A11055 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 539.6 |
| Formula | C30H29N5O5 |
| 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. | 913376-83-7 |
| Synonyms | AMG458, AMG 458 |
| SMILES | CC1=C(C(=O)N(N1CC(C)(C)O)C2=CC=CC=C2)C(=O)NC3=NC=C(C=C3)OC4=C5C=CC(=CC5=NC=C4)OC |
溶解度
| In vitro (25°C) | DMSO | 18 mg/mL (33.35 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 15% Captisol+citrate vehicle | 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 18.53 mL | 92.66 mL | 185.32 mL |
| 0.5 mM | 3.71 mL | 18.53 mL | 37.06 mL |
| 1 mM | 1.85 mL | 9.27 mL | 18.53 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.71 mL |
*The above data is based on the productmolecular weight 539.6 . 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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