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Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。
Targets
| Target | Value |
|---|---|
| RET | IC50: 1.5nM |
| Raf-1 | IC50: 2.5nM |
| VEGFR2 | IC50: 4.2nM |
| Kit | IC50: 7nM |
| VEGFR1 | IC50: 13nM |
| B-Raf(V600E) | IC50: 19nM |
| PDGFRβ | IC50: 22nM |
| B-Raf | IC50: 28nM |
| VEGFR3 | IC50: 46nM |
| FGFR1 | IC50: 202nM |
| Tie-2 | IC50: 311nM |
| In vitro (25°C) | DMSO | 88 mg/mL (182.26 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 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 | 20.71 mL | 103.56 mL | 207.13 mL |
| 0.5 mM | 4.14 mL | 20.71 mL | 41.43 mL |
| 1 mM | 2.07 mL | 10.36 mL | 20.71 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
*The above data is based on the productmolecular weight 482.8. 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 | A10250 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 482.8 |
| Formula | C21H15ClF4N4O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 755037-03-7 |
| SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F |
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