PF-4136309, CCR2 antagonist (TBI4261)

Description

Product Details

Formal 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

Molecular Formula: C₂₉H₃₁F₃N₆O₃

Formula Weight: 568.60

CAS Number: 1341224-83-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

CCR2 antagonist

Functions

PF-4136309 (1341224-83-6) is a potent (hIC50 = 5.2 nM, mIC50 = 13 nM, rIC50 = 17 nM) and selective inhibitor of CCR2. PF-4136309 significantly decreased inflammatory monocytes in a mouse model of pancreatic cancer. 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.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.