3029608-57-6
Chemical Structure
CDK12/13-IN-3
- CAS No.: 3029608-57-6
- Formula:C19H22ClN7O2
- Molecular Weight:415.88
InChIKey: BMUSKHUHESQMIP-GFCCVEGCSA-N
SMILES: COC1=NC(N[C@@H]2CCN(C3=NC=NC4=C3CCN(C(C=C)=O)C4)C2)=NC=C1Cl
Biological Activity: CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6%[1].
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CDK12/13-IN-3 | 99.14% | CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6%. | ||||||||||||||||||||
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