2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK12/13-IN-3

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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CDK12/13-IN-3 Chemical Structure

CDK12/13-IN-3 Chemical Structure

CAS No. : 3029608-57-6

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CDK12/13-IN-3 Related Antibodies

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Description

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].

IC50 & Target

CDK13

79.4 nM (IC50)

CDK12

107.4 nM (IC50)

Molecular Weight

415.88

Formula

C19H22ClN7O2
CAS No.
SMILES

COC1=NC(N[C@@H]2CCN(C3=NC=NC4=C3CCN(C(C=C)=O)C4)C2)=NC=C1Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK12/13-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK12/13-IN-33029608-57-6CDKCyclin dependent kinaseorally activeOCI-AML-3MV4?11KARPAS-299NAMALWADLD-1SW403HCT116HCC1395MDA-MB-231Inhibitorinhibitorinhibit

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