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CDK12/13-IN-3

CAT: 0804-HY-173059-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-173059-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
3029608-57-6
UNSPSC
12352005
Target
CDK
Related Pathways
Cell Cycle/DNA Damage
Field of Research
Cancer
Smiles
COC1=NC(N[C@@H]2CCN(C3=NC=NC4=C3CCN(C(C=C)=O)C4)C2)=NC=C1Cl
Molecular Formula
C19H22ClN7O2
Molecular Weight
415.88
References & Citations
[1]Lu H, et al., Design, Synthesis, and Biological Evaluation of Novel Orally Available Covalent CDK12/13 Dual Inhibitors for the Treatment of Tumors. J Med Chem. 2025 Feb 27;68 (4) :4148-4167.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CDK12; CDK13

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