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Derazantinib (ARQ-087)是成纤维细胞生长因子受体（FGFR）的口服生物利用抑制剂，对于FGFR2的IC50值为1.8 nM，对于FGFR1和3的IC50值为4.5 nM，对FGFR4的效力较低（IC50 = 34 nM）。它还抑制RET，DDR2，PDGFRβ，VEGFR和KIT。
| In vitro | DMSO | 80 mg/mL (170.73 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
|
* <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 | 21.34 mL | 106.71 mL | 213.42 mL |
| 0.5 mM | 4.27 mL | 21.34 mL | 42.68 mL |
| 1 mM | 2.13 mL | 10.67 mL | 21.34 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
*The above data is based on the productmolecular weight 468.57. 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 | A16825 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 468.57 |
| Formula | C29H29FN4O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1234356-69-4 |
| Synonyms | ARQ087, ARQ 087 |
| SMILES | COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1 |
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