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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,670 | 6-8 weeks | |
50 mg | $2,180 | 6-8 weeks | |
100 mg | $2,800 | 6-8 weeks |
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). |
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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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