Chemical Name: N-[2-[(3S)-3-[[4-Hydroxy-4-(5-pyrimidin-2-ylpyridin-2-yl)cyclohexyl]amino]pyrrolidin-1-yl]-2-oxoethyl]-3-(trifluoromethyl)benzamide. Alternate Names: INCB8761
CCR2 antagonist
Molecular Weight:
568.60
Purity:
98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1341224-83-6]
Formula:
C29H31F3N6O3
Application Notes:
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
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