纯度:98% by HPLC;NMR (Conforms)
分子式:C29H31F3N6O3
分子量:568.60
溶剂:DMSO (>25 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):CCR2 antagonist
Function / Pharmacology:PF-4136309 (1341224-83-6) is a potent (hIC50 = 5.2 nM, mIC50 = 13 nM, rIC50 = 17 nM) and selective inhibitor of CCR2.1 PF-4136309 significantly decreased inflammatory monocytes in a mouse model of pancreatic cancer.2 In combination therapy with the FOLFIRINOX regimen, PF-4136309 reversed immune suppression in the tumor microenvironment causing an influx of tumor infiltrating lymphocytes leading to overall enhanced efficacy in a phase 1b study.3