INCB8761(PF-4136309) Property

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)

pka

13.17±0.46(Predicted)

form 

solid

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

HS Code 

2933998090

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

INCB8761(PF-4136309) Chemical Properties,Usage,Production

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.

Uses

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