生物活性
Apatinib (YN968D1)是一种酪氨酸激酶抑制剂，可选择性抑制血管内皮生长因子受体2（VEGFR2，也称为KDR），后者可抑制VEGF介导的内皮细胞迁移和增殖，从而阻止肿瘤组织中新血管的形成。
Targets
| Target | Value |
| VEGFR2 | IC50: 1nM |
| RET | IC50: 13nM |
| c-Kit | IC50: 429nM |
| c-Src | IC50: 530nM |
| PDGFRα | IC50: >1μM |
| EGFR | IC50: >10μM |
| HER2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
化学数据
| 目录号 | A11407 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 493.6 |
| Formula | C25H27N5O4S |
| 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. | 811803-05-1 |
| SMILES | CS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4 |
溶解度
| In vitro | DMSO | 77 mg/mL (193.72 mM) |
| Water | Insoluble |
| Ethanol | 10 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 | 20.26 mL | 101.3 mL | 202.59 mL |
| 0.5 mM | 4.05 mL | 20.26 mL | 40.52 mL |
| 1 mM | 2.03 mL | 10.13 mL | 20.26 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.05 mL |
*The above data is based on the productmolecular weight 493.6 . 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.
