CDK8/19-IN-1
| 中文名称 | CDK8/19-IN-1 |
|---|---|
| 中文同义词 | 化合物 T10739 |
| 英文名称 | CDK8/19-IN-1 |
| 英文同义词 | CDK8/19-IN-1;CDK8/19IN1,CDK-8/19-IN-1,CDK8/19 IN 1;Thieno[3,4-g]-1,2-benzisothiazole-6-carboxamide, 4,5-dihydro-8-[[6-[[(2-methoxyethyl)amino]carbonyl]-3-pyridinyl]oxy]- |
| CAS号 | 1818427-07-4 |
| 分子式 | C19H18N4O4S2 |
| 分子量 | 430.5 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1818427-07-4.mol |
| 结构式 |  |
CDK8/19-IN-1 性质
| 沸点 | 628.9±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.432±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 13.06±0.46(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至浅黄色 |
|
CDK8/CycC 0.46 nM (IC 50 ) |
CDK19/CycC 0.99 nM (IC 50 ) |
CDK9 270 nM (IC 50 ) |
CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC 50 s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. CDK8/19-IN-1 also weakly inhibits CDK2, with 62% inhibition at 1 μM. CDK8/19-IN-1 (1 μM) shows >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, CDC7. CDK8/19-IN-1 shows K d s of 25, 46, 81, 86, 97, 160 and >3000 nM for CDK19, CDK8, DYRK1B, HASPIN, YSK4, HIPK1 and EPHA3, respectively. CDK8/19-IN-1 displays potent antitumor activity, with GI 50 of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells.
CDK8/19-IN-1 (52h; 1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth in mice bearing RPMI8226 human hematopoietic and lymphoid cells.