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Biological Activity
KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor that inhibits PDGFR-α and c-Kit at higher concentrations only (IC50 = 0.97 μM and 4.33 μM, respectively) and inactive towards 17 other kinases (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.
| Catalog Num | A10504 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 286370-15-8 |
| Formula | C20H21ClN4O4 |
| M. Wt | 416.9 |
| Purity | >98% |
| Synonyms | KRN633, KRN-633 |
| SMILES | CCCNC(=O)NC1=C(C=C(C=C1)OC2=NC=NC3=CC(=C(C=C32)OC)OC)Cl |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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