INCB8761(PF-4136309)
- Product Name
- 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);PF-4136309, 10 mM in DMSO;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
- CBNumber
- CB62627975
- Molecular Formula
- C29H31F3N6O3
- Formula Weight
- 568.59
- MOL File
- 1341224-83-6.mol
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.
N-Bromosuccinimide Price
- Product number
- 21965
- Product name
- INCB 8761
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 21965
- Product name
- INCB 8761
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 21965
- Product name
- INCB 8761
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 21965
- Product name
- INCB 8761
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- CS-0610
- Product name
- PF-4136309
- Purity
- 99.59%
- Packaging
- 100mg
- Price
- $760
- Updated
- 2021/12/16
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 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.
in vivo
PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species[1].
IC 50
Human CCR2: 5.2 nM (IC50); Mouse CCR2: 13 nM (IC50); Rat CCR2: 17 nM (IC50)
References
[1] CHU-BIAO XUE*. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist[J]. ACS Medicinal Chemistry Letters, 2011, 2 12: 913-918. DOI:10.1021/ml200199c
[2] DOMINIC E SANFORD. Inflammatory monocyte mobilization decreases patient survival in pancreatic cancer: a role for targeting the CCL2/CCR2 axis.[J]. Clinical Cancer Research, 2013, 19 13: 3404-3415. DOI:10.1158/1078-0432.ccr-13-0525
[3] Phase 1b study targeting tumor associated macrophages with CCR2 inhibition plus FOLFIRINOX in locally advanced and borderline resectable pancreatic cancer
INCB8761(PF-4136309) Preparation Products And Raw materials
Raw materials
Preparation Products
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