生物活性
RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。
靶点信息
| VEGFR2 (Cell-free assay) | B-Raf (Cell-free assay) | | | |
| 30 nM(EC50) | 3 nM-60 nM | | | |
化学数据
| 目录号 | A10773 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 518.4 |
| Formula | C24H16F6N6O |
| 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. | 927880-90-8 |
| SMILES | CN1C2=C(C=C(C=C2)OC3=CC(=NC=C3)C4=NC=C(N4)C(F)(F)F)N=C1NC5=CC=C(C=C5)C(F)(F)F |
溶解度
| In vitro (25°C) | DMSO | 85 mg/mL (163.96 mM) |
| Water | Insoluble |
| Ethanol | 28 mg/mL (54.01 mM) |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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 | 19.29 mL | 96.45 mL | 192.9 mL |
| 0.5 mM | 3.86 mL | 19.29 mL | 38.58 mL |
| 1 mM | 1.93 mL | 9.65 mL | 19.29 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
*The above data is based on the productmolecular weight 518.4 . 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.
