ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Mitogen-activated protein kinase (MAPK) >Raf inhibitors >PLX-4720

PLX-4720

PLX-4720 Structure
CAS No.
918505-84-7
Chemical Name:
PLX-4720
Synonyms
PLX-4720;CS-1917;PLX4720, >=98%;(+-)-Oxypeucedanin;Raf Kinase Inhibitor V;PLX-4720;PLX 4720;PLX4720;N-[3-[(5-Chloro-1H-pyrrol...;PLX-4720;PLX 4720;PLX4720;RAF KINASE INHIBITOR V;N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-dif...;N-[3-(5-Chloro-7-azaindole-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide
CBNumber:
CB72484744
Molecular Formula:
C17H14ClF2N3O3S
Molecular Weight:
413.83
MOL File:
918505-84-7.mol
MSDS File:
SDS
Modify Date:
2023/10/26 14:41:44

PLX-4720 Properties

Melting point 230-233oC
Density 1.55
storage temp. +2C to +8C
solubility DMSO (Slightly), Methanol (Slightly, Heated)
form Orange-yellow solid
pka 6.20±0.10(Predicted)
color White to Off-White

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

PLX-4720 Chemical Properties,Uses,Production

Description

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. Mutations in the kinase B-Raf are involved in a wide range of cancers. In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf. PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM). It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases. PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

Definition

ChEBI: A pyrrolopyridine that is vemurafenib in which the p-chlorophenyl group has been replaced by chlorine. It is a potent and selective inhibitor of the Raf kinase B-Raf(V600E).

Advantages

PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases, and potent cytotoxic effects are also exclusive to cells bearing the V600E allele. Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E-bearing tumor cell lines but not in cells lacking oncogenic B-Raf. In melanoma models, PLX4720 induces cell cycle arrest and apoptosis exclusively in B-RafV600E-positive cells. In B-RafV600E-dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity[1].

PLX-4720 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 189)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Capot Chemical Co.,Ltd. 571-85586718 +8613336195806 China 29798 60 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29901 58 Inquiry
Shenzhen Nexconn Pharmatechs Ltd +86-755-89396905 +86-15013857715 China 10259 58 Inquiry
Chongqing Chemdad Co., Ltd +86-023-6139-8061 +86-86-13650506873 China 39916 58 Inquiry
CONIER CHEM AND PHARMA LIMITED +8618523575427 China 49391 58 Inquiry
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 United States 19892 58 Inquiry
Shanghai Gubang New Materail Technology Co. LTD 21-51317962 +8618721305404 CHINA 272 58 Inquiry
1-PropanesulfonaMide, N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]- N-[3-[(5-Chloro-1H-pyrrol... N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide PLX 4720 PLX 4720 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide PLX4720, >=98% Raf Kinase Inhibitor V PLX-4720, N-(3-(5-Chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide N-(3-(5-Chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide PLX-4720;PLX 4720;PLX4720;RAF KINASE INHIBITOR V CS-1917 PLX-4720;PLX 4720;PLX4720 Propane-1-sulfonic acid [3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide (PLX4720) N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide USP/EP/BP N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-dif... (+-)-Oxypeucedanin PLX-4720 N-[3-(5-Chloro-7-azaindole-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide 918505-84-7 918595-84-7 C17H7D7ClF2N3O3S C17H14ClF2N3O3S C17H14O3N3SF2Cl Inhibitors MAPK Aromatics Heterocycles Intermediates & Fine Chemicals Isotope Labelled Compounds Pharmaceuticals Sulfur & Selenium Compounds