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| | INCB8761(PF-4136309) Basic information |
| Product Name: | INCB8761(PF-4136309) | | Synonyms: | 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) | | CAS: | 1341224-83-6 | | MF: | C29H31F3N6O3 | | MW: | 568.59 | | EINECS: | | | Product Categories: | | | Mol File: | 1341224-83-6.mol |  |
| | INCB8761(PF-4136309) Chemical 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. |
| | INCB8761(PF-4136309) Usage And Synthesis |
| 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 |
| | INCB8761(PF-4136309) Preparation Products And Raw materials |
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