Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,670.00 | |
50 mg | 6-8 weeks | $ 2,180.00 | |
100 mg | 6-8 weeks | $ 2,800.00 |
Description | CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9). |
Targets&IC50 | CDK19-CyclinA:0.99 nM, CDK8-CyclinC:0.46 nM, CDK9:270 nM |
In vitro | CDK8/19-IN-1 (52h) 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 (GI50: 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells). |
In vivo | In mice bearing RPMI8226 human hematopoietic and lymphoid cells, CDK8/19-IN-1 (1.25 mg/kg twice daily or 2.5 mg/kg once daily, p.o.) significantly suppresses tumor growth. |
Molecular Weight | 430.5 |
Formula | C19H18N4O4S2 |
CAS No. | 1818427-07-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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CDK8/19-IN-1 1818427-07-4 Cell Cycle/Checkpoint CDK CDK8/19IN1 CDK-8/19-IN-1 CDK8/19 IN 1 inhibitor inhibit