Factory price PLX4032 CAS 918504-65-1 in stock

Details:

Factory price PLX4032 CAS 918504-65-1 in stock

Details

PLX4032 Basic information
Product Name:    PLX4032
Synonyms:    N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide;PLX4032 (VeMurafenib);PLX4032, RG7204, ZELBORAF, RO5185426;R7204;N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaM;PLX4032, R7204, RG7204, RO5185426;VeMurafenib (PLX4032, RG7204);N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide Vemurafenib PLX 4032
CAS:    918504-65-1
MF:    C23H18ClF2N3O3S
MW:    489.92
EINECS:    
Product Categories:    API;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators;Sulfur & Selenium Compounds;Aromatics;Inhibitor;RG7204;Antineoplastic;Inhibitors;MAPK
Mol File:    918504-65-1.mol
PLX4032 Structure
PLX4032 Chemical Properties
density     1.46
storage temp.     -20°C
solubility     Soluble in DMSO (up to 100 mg/ml)
form     White powder.
pka    6.26±0.10(Predicted)
color     White or 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.
CAS DataBase Reference    918504-65-1
Safety Information
HS Code     29339900
Hazardous Substances Data    918504-65-1(Hazardous Substances Data)
MSDS Information
PLX4032 Usage And Synthesis
Description    In August 2011, the United States FDA approved vemurafenib (PLX- 4032, RO-5185426) for the treatment of patients with metastatic melanoma with the BRAFV600E mutation. Vemurafenib has been developed as a targeted therapy for patients with the BRAF gene mutation since oncogenic B-raf signaling is implicated in approximately 50% of melanomas. Vemurafenib was identified based on an initial high-throughput screen followed by the extensive use of structure-based drug design. Vemurafenib is a potent inhibitor of B-RafV600E kinase (IC50=13 nM) compared to its potency against wildtype B-raf (IC50=160 nM) and is fairly selective versus a panel of 200 kinases. It does inhibit other kinases (RAF1, SRMS, ACK1, MAP4K5, and FGR) and mutant B-raf kinases (BRAFV600K, BRAFV600D, and BRAFV600R) with enzyme IC50's of <100 nM.
Chemical Properties    Off-White Solid
Originator    Plexxikon (United States)
Uses    Vemurafenib selective BRAFV600E kinase inhibitor; an antitumor agent. Vemurafenib functions by inhibiting the proliferation and mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase and ERK phosphorylation in a panel of tumor cell lines, including melanoma cell lines expressing BRAFV600E or other mutant BRAF proteins altered at codon 600.
Uses    Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM
Uses    PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively). It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells. PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.[Cayman Chemical]
Definition    ChEBI: A pyrrolopyridine that is 1H-pyrrolo[2,3-b]pyridine which is substituted at position 5 by a p-chlorophenyl group and at positions 3 by a 3-amino-2,6-difluorobenzoyl group, the amino group of which has undergone ormal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases.

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