生物活性
Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。
靶点信息
| PDGFRα (CHO cells) | PDGFRβ (CHO cells) | FLT3 | | |
| 2.1 nM(Kd) | 3.2 nM(Kd) | 0.74 nM (Kd) | | |
化学数据
| 目录号 | A11052 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 443.5 |
| Formula | C26H29N5O2 |
| 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. | 670220-88-9 |
| Synonyms | CP868596, CP 868596 |
| SMILES | CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 84 mg/mL (189.38 mM) |
| Water | Insoluble |
| Ethanol | 7 mg/mL (15.78 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 | 22.55 mL | 112.74 mL | 225.48 mL |
| 0.5 mM | 4.51 mL | 22.55 mL | 45.1 mL |
| 1 mM | 2.25 mL | 11.27 mL | 22.55 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.51 mL |
*The above data is based on the productmolecular weight 443.5 . 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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