LEE011 (succinate)

LEE011 is a cyclin-dependent kinase 4 (Cdk4) and Cdk6 inhibitor (IC50s = 0.53 and 2.3 nM, respectively). It is selective for Cdk4/6 over Cdk1, Cdk2, Cdk5, Cdk7, and Cdk9 (IC50s = >1,400, >2,500, >2,000, >2,000, and 190 nM, respectively). LEE011 reduces the proliferation of MCF-7 and T47D breast cancer cells (IC50s = 200 and 260 nM, respectively). It induces cell death in C666-1 and NPC/HK1 nasopharyngeal carcinoma cells (IC50s = 12.25 and 5.07 µM, respectively) and cell cycle arrest at the G0/G1 phase in the same cells when used at a concentration of 10 µM. LEE011 (200 mg/kg every two weeks), in combination with the PI3Kalpha inhibitor alpelisib (BYL719, Cay-16986), reduces tumor growth in two patient-derived xenograft (PDX) mouse models of nasopharyngeal carcinoma.Formal Name: butanedioic acid, compd. with 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide. CAS Number: 1374639-75-4. Synonyms: NVP-LEE011, Ribociclib. Molecular Formula: C23H30N8O . C4H6O4. Formula Weight: 552.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 276, 345 nm. SMILES: O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(C=C4)=NC=C4N5CCNCC5.O=C(CCC(O)=O)O. InChi Code: InChI=1S/C23H30N8O.C4H6O4/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30,5-3(6)1-2-4(7)8/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28),1-2H2,(H,5,6)(H,7,8). InChi Key: NHANOMFABJQAAH-UHFFFAOYSA-N.