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KRN 633是一种细胞可渗透、可逆、ATP竞争性VEGFR激酶抑制剂，仅在较高浓度下(IC50 = 0.97 μM和4.33 μM)抑制PDGFR-α和C-Kit，对其他17种激酶无活性(IC50 ≥ 10 μM)。
Targets
| Target | Value |
|---|---|
| VEGFR3 | IC50: 125nM |
| VEGFR2 | IC50: 160nM |
| VEGFR1 | IC50: 170nM |
| PDGFRα | IC50: 965nM |
| c-Kit | IC50: 4330nM |
| BTK | IC50: 9200nM |
| PDGFRβ | IC50: 9850nM |
| Tie-2 | IC50: 9900nM |
| In vitro (25°C) | DMSO | 8 mg/mL (19.18 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 0.5% methylcellulose+0.2% Tween 80 | 9 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 | 23.99 mL | 119.93 mL | 239.87 mL |
| 0.5 mM | 4.8 mL | 23.99 mL | 47.97 mL |
| 1 mM | 2.4 mL | 11.99 mL | 23.99 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.8 mL |
*The above data is based on the productmolecular weight 416.9. 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 | A10504 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 416.9 |
| Formula | C20H21ClN4O4 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 286370-15-8 |
| Synonyms | KRN633, KRN-633 |
| SMILES | CCCNC(=O)NC1=C(C=C(C=C1)OC2=NC=NC3=CC(=C(C=C32)OC)OC)Cl |
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