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CDK8/19-IN-1 is a selective, orally bioavailable dual inhibitor of CDK8 and CDK19, with IC50 values of 0.46 nM for CDK8, 0.99 nM for CDK19, and 270 nM for [CDK9].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,670 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $2,180 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,800 | 6-8 weeks | 6-8 weeks |
| Description | CDK8/19-IN-1 is a selective, orally bioavailable dual inhibitor of CDK8 and CDK19, with IC50 values of 0.46 nM for CDK8, 0.99 nM for CDK19, and 270 nM for [CDK9]. |
| Targets&IC50 | CDK8-CyclinC:0.46 nM, CDK19-CyclinA:0.99 nM, CDK9:270 nM |
| In vitro | CDK8/19-IN-1 (52h) weakly inhibits CDK2, achieving 62% inhibition at 1 μM. At 1 μM, it exhibits >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, and CDC7. The compound shows dissociation constants (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 demonstrates potent antitumor activity with GI50 values ranging from 0.43 to 2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), and 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 |
| Smiles | O(C1=C2C(=C(C(N)=O)S1)CCC3=C2SN=C3)C=4C=CC(C(NCCOC)=O)=NC4 |
| Relative Density. | 1.432 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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