1818427-07-4
1818427-07-4 structure
- Name: CDK8/19-IN-1
- Chemical Name: CDK8/19-IN-1
- CAS Number: 1818427-07-4
- Molecular Formula: C19H18N4O4S2
- Molecular Weight: 430.50
- Catalog: Research Areas Cancer
- Create Date: 2019-02-11 07:18:51
- Modify Date: 2024-01-13 12:35:14
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CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
| Name | CDK8/19-IN-1 |
|---|
| Description | CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. |
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| Related Catalog | |
| Target |
CDK8/CycC:0.46 nM (IC50) CDK19/CycC:0.99 nM (IC50) CDK9:270 nM (IC50) |
| In Vitro | CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC50s 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 Kds 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 GI50 of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells[1]. |
| In Vivo | 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[1]. |
| References |
| Molecular Formula | C19H18N4O4S2 |
|---|---|
| Molecular Weight | 430.50 |