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CDK8/19-IN-51
🥰Excellent
Catalog No. T22633Cas No. 1860885-61-5
Alias CCT251545 analogue, Compound 51
CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.
CDK8/19-IN-51
🥰Excellent
Purity: 98.65%
Catalog No. T22633Alias CCT251545 analogue, Compound 51Cas No. 1860885-61-5
CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $530 | In Stock | |
| 5 mg | $1,170 | In Stock | |
| 10 mg | $1,660 | In Stock | |
| 25 mg | $2,158 | In Stock |
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Purity:98.65%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers. |
| Targets&IC50 | CDK19:5.6 nM, p-STAT1727:17.9 nM, CDK8:5.1 nM, 7dF3:7.2 nM |
| In vitro | In SW620 human colorectal carcinoma cells harboring an activating APC mutation, CDK8/19-IN-51 inhibited phospho-STAT1^Ser727 with an IC50 of 17.9 nM, which serves as a biomarker of CDK8 inhibition [1]. |
| In vivo | In in vivo pharmacokinetic (PK) studies in mice and rats, CDK8/19-IN-51 exhibited moderate in vivo clearance and volume of distribution (Vd) but showed low bioavailability in mice. In an SW620 human colorectal carcinoma xenograft model, oral administration of CDK8/19-IN-51 (5 mg/kg) inhibited phospho-STAT1^Ser727 in a time-dependent manner. CDK8/19-IN-51 serves as an advanced chemical tool for further investigation of the efficacy, safety, and tolerability of dual CDK8/19 inhibitors [1]. |
| Alias | CCT251545 analogue, Compound 51 |
| Molecular Weight | 414.46 |
| Formula | C23H22N6O2 |
| Cas No. | 1860885-61-5 |
| Smiles | O=C(C1=NC2=C(C=NC(N)=C2C=C1)C3=CC=C(C=C3)C=4C=NN(C4)C)N5CC(OC)C5 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 8.00 mg/mL (19.30 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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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
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