生物活性
Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。
靶点信息
| Abl (Cell-free assay) | Src (Cell-free assay) | c-Kit (D816V) (Cell-free assay) | c-Kit (wt) (Cell-free assay) | |
| 0.6 nM | 0.8 nM | 37 nM | 79 nM | |
化学数据
| 目录号 | A10290 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 488.0 |
| Formula | C22H26ClN7O2S |
| 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. | 302962-49-8 |
| Synonyms | Sprycel |
| SMILES | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=NC(=NC(=C3)N4CCN(CC4)CCO)C |
溶解度
| In vitro (25°C) | DMSO | 84 mg/mL (172.12 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O | 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 | 20.49 mL | 102.46 mL | 204.92 mL |
| 0.5 mM | 4.1 mL | 20.49 mL | 40.98 mL |
| 1 mM | 2.05 mL | 10.25 mL | 20.49 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.1 mL |
*The above data is based on the productmolecular weight 488.0 . 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.
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