abemaciclib-ly2835219-mesylate

Description: Abemaciclib mesylate (formerly known as LY2835219; trade name: Verzenio) is a potent and selective, orally available dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. In September 2017, Abemaciclib was approved by FDA to treat certain advanced or metastatic breast cancers. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6 can cause cell cycle deregulation as seen in certain types of cancer.

References: Oncotarget. 2016 Mar 22; 7(12):14803-13; Biochem Pharmacol. 2017 Jan 15; 124:29-42.

Related CAS#: 1231930-82-7 (mesylate salt); 1231929-97-7 (free base);

Abemaciclib; LY-2835219 mesylate; LY2835219; LY 2835219; Abemaciclib mesylate;

Chemical Name: N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine mesylate

SMILES Code: CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C.OS(=O)(C)=O

Exact Mass: 602.2599