Formulation: A solid
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
Purity: ≥98%
Formula Markup: C23H30N8O • C4H6O4
Formula Weight: 552,6
Shelf life (days): 1460
CAS Number: 1374639-75-4
Notes: LEE011 is a cyclin-dependent kinase 4 (Cdk4) and Cdk6 inhibitor (IC50s = 0.53 and 2.3 nM, respectively).{64974} 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.{64973} LEE011 (200 mg/kg every two weeks), in combination with the PI3Kα inhibitor alpelisib (BYL719; Item No. 16986), reduces tumor growth in two patient-derived xenograft (PDX) mouse models of nasopharyngeal carcinoma.
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