纯度:>98% by HPLC;NMR (Conforms)
分子式:C27H32F2N8·CH3SO3H
分子量:602.70
溶剂:DMSO > 25 mg/ml Water > 25 mg/ml
性状:Off-white solid
存储:-20°C
Activity (short version):CDK 4/6 inhibitor
Function / Pharmacology:Abemaciclib (1231930-82-7) is a potent and selective CDK4/6 inhibitor (IC50 = 2 nM and 10 nM respectively).1 It caused G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells. Abemaciclib was also active in several human tumor xenograft models. It displayed efficacy in patients with various solid tumors including breast cancer, non-small cell lung cancer, glioblastoma, melanoma, colorectal cancer, and hormone receptor-positive breast cancer.2 Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells.3 FDA approved for the treatment of advanced breast cancers.