生物活性
VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。
靶点信息
| Aurora A (Cell-free assay) | Aurora C (Cell-free assay) | Aurora B (Cell-free assay) | FLT3 (Cell-free assay) | Bcr-Abl (Cell-free assay) |
| 0.6 nM(Ki app) | 4.6 nM(Ki app) | 18 nM(Ki app) | 30 nM(Ki) | 30 nM(Ki) |
化学数据
| 目录号 | A10981 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 464.6 |
| Formula | C23H28N8OS |
| 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. | 639089-54-6 |
| SMILES | CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)SC4=CC=C(C=C4)NC(=O)C5CC5 |
溶解度
| In vitro (25°C) | DMSO | 90 mg/mL (193.71 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+30% PEG 300+2% Tween 80+ddH2O | 14 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 | 21.52 mL | 107.62 mL | 215.24 mL |
| 0.5 mM | 4.3 mL | 21.52 mL | 43.05 mL |
| 1 mM | 2.15 mL | 10.76 mL | 21.52 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
*The above data is based on the productmolecular weight 464.6 . 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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