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TCS ERK 11e (VX-11e)是一种有效且选择性的细胞外信号相关激酶2（ERK2）抑制剂（ERK2，GSK-3，Aurora激酶A和Cdk2的Ki值分别<2、395、540和852 nM）。有效阻断HT29细胞的增殖（IC50 = 48 nM）。
Targets
| Target | Value |
|---|---|
| ERK2 | ki: <2nM |
| GSK3 | ki: 400nM |
| AURA | ki: 540nM |
| CDK2 | ki: 850nM |
| FLT3 | ki: 1.4μM |
| ROCK1 | ki: 1.4μM |
| JNK3 | ki: 1.4μM |
| TAK1 | ki: 3μM |
| PKA | ki: >4μM |
| SRC | ki: >4μM |
| JAK2 | ki: >4μM |
| JAK3 | ki: >4μM |
| SYK | ki: >4μM |
| MET | ki: >4μM |
| IRAK4 | ki: >4μM |
| AKT3 | ki: >4μM |
| KDR | ki: >4μM |
| MEK1 | ki: >4μM |
| P38α | ki: >4μM |
| COT | ki: >4μM |
| ITK | ki: >4μM |
| MEKK3 | ki: >4μM |
| PLK1 | ki: >4μM |
| ZAP70 | ki: >4μM |
| IKki: ki: >5μM | |
| NIK | ki: >5μM |
| CIT | ki: >10μM |
| FAK | ki: >10μM |
| In vitro | DMSO | 94 mg/mL (187.87 mM) | |
| Water | Insoluble | ||
| Ethanol | 15 mg/mL (29.97 mM) | ||
|
* <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 | 19.99 mL | 99.93 mL | 199.86 mL |
| 0.5 mM | 4 mL | 19.99 mL | 39.97 mL |
| 1 mM | 2 mL | 9.99 mL | 19.99 mL |
| 5 mM | 0.4 mL | 2 mL | 4 mL |
*The above data is based on the productmolecular weight 500.35. 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 | A12505 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 500.35 |
| Formula | C24H20Cl2FN5O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 896720-20-0 |
| SMILES | CC1=CN=C(N=C1C2=CNC(=C2)C(=O)N[C@H](CO)C3=CC(=CC=C3)Cl)NC4=C(C=C(C=C4)F)Cl |
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