INCB8761(PF-4136309)

CAS NO.：1341224-83-6
Empirical Formula: C29H31F3N6O3
Molecular Weight: 568.59
MDL number: MFCD22124474
SAFETY DATA SHEET (SDS)
Update Date: 2026-04-24 14:58:52

What is INCB8761(PF-4136309)?

Description

PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC₅₀s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively). It also inhibits the voltage-gated potassium channel subtype K_v11.1 by 35% when used at a concentration of 10 μM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC₅₀ value of 3.9 nM.

The Uses of INCB8761(PF-4136309)

PF 4136309 is a CCR5 receptor antagonists that contributes to the treatment of rheumatoid arthritis.

References

1) Chu-Biao?et al.?(2011),?Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist;?ACS Med. Chem. Lett.?2?913 2) Sanford?et al.?(2013),?Inflammatory monocyte mobilization decreases patient survival in pancreatic cancer: a role for targeting the CCL2/CCR2 axis;?Clin. Cancer Res.?19?3404 3) Nywenig?et al.?(2016),?Phase 1b study targeting tumor associated macrophages with CCR2 inhibition plus FOLFIRINOX in locally advanced and borderline resectable pancreatic cancer;?Lancet Oncol.?17?651

Properties of INCB8761(PF-4136309)

Boiling point:	712.2±60.0 °C(Predicted)
Density	1.40±0.1 g/cm3(Predicted)
storage temp.	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility	Soluble in DMSO (up to at least 25 mg/ml)
form	solid
pka	13.17±0.46(Predicted)
color	Off-white
Stability:	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety information for INCB8761(PF-4136309)

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.