PF-4136309 | CCR2 antagonist
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $290.00 |
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
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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
References/Citations:
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
Related products
-
P5091 | DUB USP7 inhibitor
From $60.00CAS:882257-11-6Catalog Number:10-1422Activity:DUB USP7 inhibitorChemical Name:1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanoneMolecular Weight:348.23Molecular Formula:C12H7Cl2NO3S2Solubility:Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 40 mg/ml with warming).Physical Properties:White solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:RTStability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.Shipping Code:RT -
Alsterpaullone | GSK-3ß inhibitor
From $56.00CAS:237430-03-4Catalog Number:10-1397Activity:GSK3β inhibitor, CDK5/p25 inhibitorChemical Name:9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5)-oneMolecular Weight:293.28Molecular Formula:C16H11N3O3Solubility:Soluble in DMSO (up to 10 mg/ml).Physical Properties:Brown solidPurity:96% by TLC
NMR (Conforms)Storage Temperature:RTStability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.Shipping Code:RT -
TRIM | Nitric oxide synthase inhibitor
From $35.00CAS:25371-96-4Catalog Number:10-2699Activity:Nitric oxide synthase inhibitorChemical Name:1-(2-Trifluoromethylphenyl)imidazoleMolecular Weight:212.18Molecular Formula:C107F3N2Solubility:Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to 20 mg/ml).Physical Properties:White solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:RT (des.)Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
