CDK2-IN-47 

CDK2-IN-47 is a potent CDK2 inhibitor with an IC₅₀ of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer^[1].

CDK2-IN-47 (Compound 14c) (72 h) exhibits outstanding anticancer activity against MCF-7 (IC₅₀ = 0.7 μM), HCT-116 (IC₅₀ = 1.1 μM), and MGC-803 (IC₅₀ = 1.5 μM) cell lines, coupled with remarkable selectivity over non-cancerous HEK293 cells (SI = 22.4)^[1].
CDK2-IN-47 (0.7 μM, 48 h) induces significant apoptosis in MCF-7 cells^[1].
CDK2-IN-47 (0.7 μM, 24 h) induces G0/G1 phase phase arrest in MCF-7 cells^[1].
CDK2-IN-47 leads to a significant reduction in Rb phosphorylation at Ser807/811 in MCF-7 cells^[1].
CDK2-IN-47 demonstrates high metabolic stability in human liver microsomes (t_½ = 68.5 min, CLint = 8.5 mL/min/kg)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

381.45

C₁₆H₂₃N₅O₄S

O=C1C(C)=CN(CC(N[C@H](CC(C)C)C(OC)=O)=O)C2=NC(SC)=NN12

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nagy IM, et al. Design, synthesis, biological and computational evaluation of novel S/N-glycerolyl and peptide-conjugated [1,2,4]triazolo[1,5-a]pyrimidine derivatives as potent CDK2 inhibitors for anticancer therapy. Bioorg Chem. 2025 Sep 2;165:108952.  [Content Brief]