CDK12-IN-E9

• CAT Number: I017214
• CAS Number: 2020052-55-3
• Molecular Formula: C₂₄H₃₀N₆O₂
• Molecular Weight: 434.53
• Purity: ≥95%
• IUPAC Name: N-[3-[[3-ethyl-5-[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]phenyl]prop-2-enamide
• InChI: InChI=1S/C24H30N6O2/c1-3-17-16-25-30-22(26-18-8-7-9-19(14-18)27-23(32)4-2)15-21(28-24(17)30)29-12-6-5-10-20(29)11-13-31/h4,7-9,14-16,20,26,31H,2-3,5-6,10-13H2,1H3,(H,27,32)/t20-/m0/s1
• InChIKey: CDCHESFKYUNJPV-FQEVSTJZSA-N
• SMILES: CCC1=C2N=C(C=C(N2N=C1)NC3=CC(=CC=C3)NC(=O)C=C)N4CCCC[C@H]4CCO

CDK12-IN-E9（Cat No.:I017214）is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), which plays a critical role in transcription regulation and DNA damage response. By inhibiting CDK12, this compound disrupts the transcription of genes involved in DNA repair, leading to increased sensitivity of cancer cells to DNA-damaging agents. CDK12-IN-E9 has shown promise in preclinical studies, particularly for tumors with deficiencies in DNA repair mechanisms, such as certain breast and ovarian cancers. Ongoing research aims to evaluate its efficacy and safety, positioning it as a potential therapeutic strategy in personalized cancer treatments.

Reference

[1]. Gao Y, et al. Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.