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BGJ398 (NVP-BGJ398)是一种有效的选择性抑制剂，具有成纤维细胞生长因子受体（FGFR）酪氨酸激酶1、2、3和4的潜在抗血管生成和抗肿瘤活性（对于FGFR1，FGFR2，FGFR3，IC50值为0.9、1.4、1.0和60 nM， 和FGFR4）。
Targets
| Target | Value |
|---|---|
| FGFR1 | IC50: 0.9nM |
| FGFR3 | IC50: 1.0nM |
| FGFR2 | IC50: 1.4nM |
| FGFR3(K650E) | IC50: 4.9nM |
| FGFR4 | IC50: 60nM |
| VEGFR2 | IC50: 0.18μM |
| Lyn | IC50: 0.30μM |
| Kit | IC50: 0.75μM |
| YES | IC50: 1.1μM |
| Fyn | IC50: 1.9μM |
| Abl | IC50: 2.3μM |
| LCK | IC50: 2.5μM |
| In vitro (25°C) | DMSO | Warmed: 1 mg/mL (1.78 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1%CMC-Na | 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.84 mL | 89.21 mL | 178.42 mL |
| 0.5 mM | 3.57 mL | 17.84 mL | 35.68 mL |
| 1 mM | 1.78 mL | 8.92 mL | 17.84 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.57 mL |
*The above data is based on the productmolecular weight 560.48. 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.
| 目录号 | A11159 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 560.48 |
| Formula | C26H31Cl2N7O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 872511-34-7 |
| Synonyms | BGJ-398 |
| SMILES | CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl |
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