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Biological Activity
Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and 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. |
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| 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.
| Catalog Num | A16825 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1234356-69-4 |
| Formula | C29H29FN4O |
| M. Wt | 468.57 |
| Purity | >98% |
| Synonyms | ARQ087, ARQ 087 |
| SMILES | COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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