CDK2-IN-42

• Description :

  CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer[1].

• UNSPSC :

  12352005

• Target :

  CDK

• Related Pathways :

  Cell Cycle/DNA Damage

• Field of Research :

  Cancer

• Smiles :

  O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=CC(NC3=NC=CC(C4=CN=C(NC)S4)=N3)=C2

• Molecular Formula :

  C19H15N7O4S

• Molecular Weight :

  437.43

• References & Citations :

  [1]Cao Y, et al. Discovery of 4- (2- (methylamino) thiazol-5-yl) pyrimidin-2-amine derivatives as novel cyclin-dependent kinase 12 (CDK12) inhibitors for the treatment of esophageal squamous cell carcinoma. Bioorg Chem. 2025 May;158:108302.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CDK12