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INCB8761(PF-4136309)

CAS No.
1341224-83-6
Chemical Name:
INCB8761(PF-4136309)
Synonyms
CS-1440;EOS-61910;NCB8761(PF-4136309);INCB8761(PF-4136309);PF-04136309(INCB-8761);ZNSVOHSYDRPBGI-LXWOLXCRSA-N;N-(2-((S)-3-(((1R,4S)-4-HYDROXY-4-(5-(PYRIMIDIN-2-YL);INCB8761; PF-4136309; PF4136309; PF 4136309; INCB-8761;INCB-8761,INCB 8761,inhibit,PF-4136309,CC chemokine receptor,CCR,Inhibitor,PF4136309;N-(2-((S)-3-((trans-4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide
CBNumber:
CB62627975
Molecular Formula:
C29H31F3N6O3
Molecular Weight:
568.59
MDL Number:
MOL File:
1341224-83-6.mol
Last updated:2023-06-08 09:02:51

INCB8761(PF-4136309) Properties

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.
FDA UNII 3M2595V4KT

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338
HS Code  2933998090
NFPA 704
0
2 0

INCB8761(PF-4136309) price More Price(29)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21965 INCB 8761 1341224-83-6 1mg $32 2024-03-01 Buy
Cayman Chemical 21965 INCB 8761 1341224-83-6 5mg $139 2024-03-01 Buy
Cayman Chemical 21965 INCB 8761 1341224-83-6 10mg $243 2024-03-01 Buy
Cayman Chemical 21965 INCB 8761 1341224-83-6 25mg $533 2024-03-01 Buy
ChemScene CS-0610 PF-4136309 99.59% 1341224-83-6 100mg $760 2021-12-16 Buy
Product number Packaging Price Buy
21965 1mg $32 Buy
21965 5mg $139 Buy
21965 10mg $243 Buy
21965 25mg $533 Buy
CS-0610 100mg $760 Buy

INCB8761(PF-4136309) Chemical Properties,Uses,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 Kv11.1 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

624-28-2
1341224-83-6
Synthesis of INCB8761(PF-4136309) from 2,5-Dibromopyridine
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1341224-83-6(INCB8761(PF-4136309))Related Search:

INCB8761(PF-4136309) NCB8761(PF-4136309) PF-04136309(INCB-8761) Benzamide, N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)- EOS-61910 N-(2-((S)-3-(((1r,4S)-4-hydroxy-4-(5-(pyrimidin-2-yl) yridine-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide ZNSVOHSYDRPBGI-LXWOLXCRSA-N N-(2-((S)-3-(((1R,4S)-4-HYDROXY-4-(5-(PYRIMIDIN-2-YL) CS-1440 INCB8761; PF-4136309; PF4136309; PF 4136309; INCB-8761 N-(2-((S)-3-((trans-4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide INCB-8761,INCB 8761,inhibit,PF-4136309,CC chemokine receptor,CCR,Inhibitor,PF4136309 1341224-83-6