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MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。
Targets
| Target | Value |
|---|---|
| c-Met(M1250T) | IC50: 0.4nM |
| c-Met(Y1235D) | IC50: 0.5nM |
| c-Met(Y1230H) | IC50: 1.0nM |
| c-Met(N1100) | IC50: 1.5nM |
| c-Met(Y1230C) | IC50: 1.5nM |
| c-Met | IC50: 2.5nM |
| RON | IC50: 7nM |
| FLT1 | IC50: 10nM |
| FLT3 | IC50: 22nM |
| PDGFRβ | IC50: 22nM |
| Mer | IC50: 24nM |
| FGFR2 | IC50: 39nM |
| KDR | IC50: 44nM |
| TrkA | IC50: 46nM |
| FGFR3 | IC50: 50nM |
| TrkB | IC50: 61nM |
| FGFR1 | IC50: 65nM |
| FLT4 | IC50: 78nM |
| DRAK1 | IC50: 199nM |
| JAK2 | IC50: 225nM |
| IRAK4 | IC50: 298nM |
| MELK | IC50: 606nM |
| RET | IC50: 635nM |
| DYRK2 | IC50: 1.143μM |
| MLK1 | IC50: 4.303μM |
| IRAK1 | IC50: 5.459μM |
| Abl | IC50: 7.747μM |
| In vitro (25°C) | DMSO | 95 mg/mL (191.7 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4 | 14 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 | 20.18 mL | 100.89 mL | 201.78 mL |
| 0.5 mM | 4.04 mL | 20.18 mL | 40.36 mL |
| 1 mM | 2.02 mL | 10.09 mL | 20.18 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
*The above data is based on the productmolecular weight 495.6 . 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 | A11753 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 495.6 |
| Formula | C24H25N5O5S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 917879-39-1 |
| Synonyms | MK2461 |
| SMILES | CN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)C[C@@H]5COCCO5)C(=O)C3=C2 |
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