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CDK8/19-IN-1 

Cat. No. M28917
CDK8/19-IN-1  Structure
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Quality Control & Documentation
Biological Activity

CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

Chemical Information
Molecular Weight 430.5
Formula C19H18N4O4S2
CAS Number 1818427-07-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xiaokai Ding, et al. Proc Natl Acad Sci U S A. Inhibition of CDK8/19 Mediator kinase potentiates HER2-targeting drugs and bypasses resistance to these agents in vitro and in vivo

[2] Takanori Yamada, et al. Stem Cell Reports. The role of CDK8 in mesenchymal stem cells in controlling osteoclastogenesis and bone homeostasis

[3] Jonathan Chou, et al. Cancer Discov. Transcription-Associated Cyclin-Dependent Kinases as Targets and Biomarkers for Cancer Therapy

[4] Julie Soutourina. Nat Rev Mol Cell Biol. Transcription regulation by the Mediator complex

[5] Marcos Malumbres. Genome Biol. Cyclin-dependent kinases

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  Catalog
Abmole Inhibitor Catalog




Keywords: CDK8/19-IN-1  supplier, CDK, inhibitors, activators


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