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
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