Abemaciclib - 97%, high purity , Cyclin-dependent kinase 6 inhibitor, CAS No.1231929-97-7, Cyclin-dependent kinase 6 inhibitor

Item Number

L190223

• Synonyms: L01XE50 | 5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3H-benzimidazol-5-yl)pyrimidin-2-yl)amine | EX-A521 | LY 2835219 (free base) | NSC783671 | NSC-783671 | 5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluor
• Specifications & Purity: Moligand™, ≥97%
• Storage Temp: Protected from light,Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Cyclin-dependent kinase 6 inhibitor

Product Description

Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells.