| Name | CDK8/19-IN-51 |
| 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. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 8 mg/mL (19.3 mM), Sonication is recommended.
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| Keywords | CCT-251545 analogue, Compound 51 |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Post-Translational Modification Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | High-Efficiency Gene Editing Small Molecule Library |
United States
