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CDK8/19-IN-1
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Catalog No. T10739Cas No. 1818427-07-4
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].
CDK8/19-IN-1
😃Good
Catalog No. T10739Cas No. 1818427-07-4
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 | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,670 | 6-8 weeks | |
| 50 mg | $2,180 | 6-8 weeks | |
| 100 mg | $2,800 | 6-8 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Relative Density. | 1.432 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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