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PLX4032

PLX4032 structure

CAS No.: 918504-65-1

Chemical Name:: PLX4032

Synonyms: R7204;104532;CS-1916;Vemurafenib, >=99%;PLX4032 (VeMurafenib);Zelboraf (vemurafenib);(1029872-54-5) vemurafenib;Vemurafenib (10mM in DMSO);Vemurafenib (RG7204,PLX4032);VeMurafenib (PLX4032, RG7204)

CBNumber:: CB02550000

Molecular Formula:: C23H18ClF2N3O3S

Molecular Weight:: 489.92

MDL Number:: MFCD18074504

MOL File:: 918504-65-1.mol

MSDS File:: SDS

Last updated:2025-05-07 21:23:15

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PLX4032 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
FDA UNII	207SMY3FQT

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS09
Signal word	Warning
Hazard statements	H410
Precautionary statements	P273-P391-P501
HS Code	29339900
Hazardous Substances Data	918504-65-1(Hazardous Substances Data)

PLX4032 price More Price(32)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	10618	PLX4032 ≥98%	918504-65-1	5mg	$44	2024-03-01	Buy
Cayman Chemical	10618	PLX4032 ≥98%	918504-65-1	10mg	$70	2024-03-01	Buy
Cayman Chemical	10618	PLX4032 ≥98%	918504-65-1	25mg	$161	2024-03-01	Buy
Cayman Chemical	10618	PLX4032 ≥98%	918504-65-1	50mg	$299	2024-03-01	Buy
TRC	V118500	Vemurafenib	918504-65-1	5mg	$50	2021-12-16	Buy

Product number	Packaging	Price	Buy
10618	5mg	$44	Buy
10618	10mg	$70	Buy
10618	25mg	$161	Buy
10618	50mg	$299	Buy
V118500	5mg	$50	Buy

PLX4032 Chemical Properties,Uses,Production

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 IC_50'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.

brand name

Zelboraf

Biological Activity

Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.

in vitro

PLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation.

in vivo

In B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival.

target

B-RafV600E

storage

Store at -20°C

References

1) Khazak?et al. (2007),?Selective Raf inhibition in cancer therapy; Expert Opin. Ther. Targets,?11?1587 2) Tap?et al.?(2010),?Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma; Neoplasia,?12?637 3) Lee?et al.?(2010),?PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas; Pigment Cell Melanoma Res.,?23?820 4) Flaherty?et al.?(2010),?Inhibition of mutated, activated BRAF in metastatic melanoma; N. Engl. J. Med.,?363?809

PLX4032 Preparation Products And Raw materials

Raw materials

Preparation Products

PLX4032 Suppliers

Global( 262)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21628	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
Shandonghaohong biotechnology Co.,ltd.	0635-6175299 13961496334	sale@inyelchem.com	CHINA	44	55
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29856	58
Shanghai Arbor Chemical Co., Ltd.	021-60451682	act@arborchemical.com	CHINA	904	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22963	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19552	58
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63687	58
Shenzhen Excellent Biotech Co., Ltd.	13480692018	ramyan@ex-biotech.com	CHINA	954	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49732	58

Supplier	Advantage
Henan Tianfu Chemical Co.,Ltd.	55
ATK CHEMICAL COMPANY LIMITED	60
Shandonghaohong biotechnology Co.,ltd.	55
career henan chemical co	58
Shanghai Arbor Chemical Co., Ltd.	58
Hubei xin bonus chemical co. LTD	58
BOC Sciences	58
Alchem Pharmtech,Inc.	58
Shenzhen Excellent Biotech Co., Ltd.	58
CONIER CHEM AND PHARMA LIMITED	58

View Lastest Price from PLX4032 manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2025-05-14	N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide 918504-65-1			0.99		RongNa Biotechnology Co.,Ltd
2025-05-07	Vemurafenib 918504-65-1	US $50.00-100.00 / mg		99.65%	10g	TargetMol Chemicals Inc.
2021-07-13	Vemurafenib 918504-65-1	US $15.00-10.00 / KG	1KG	99%+ HPLC	Monthly supply of 1 ton	Zhuozhou Wenxi import and Export Co., Ltd

N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide
918504-65-1
0.99
RongNa Biotechnology Co.,Ltd

Vemurafenib
918504-65-1
US $50.00-100.00 / mg
99.65%
TargetMol Chemicals Inc.

Vemurafenib
918504-65-1
US $15.00-10.00 / KG
99%+ HPLC
Zhuozhou Wenxi import and Export Co., Ltd

PLX4032 Spectrum

PLX4032(918504-65-1)¹HNMR

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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 Zelboraf (vemurafenib) Vemurafenib, >=99% Vemurafenib (RG7204,PLX4032) RG7204;PLX-4032;PLX 4032;RG-7204 CS-1916 PLX 4032 - RG 7204 | Vemurafenib | RO 5185426 104532 (1029872-54-5) vemurafenib N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide USP/EP/BP Vemurafenib (10mM in DMSO) VemurafenibQ: What is Vemurafenib Q: What is the CAS Number of Vemurafenib Q: What is the storage condition of Vemurafenib Q: What are the applications of Vemurafenib Raf kinases,Vemurafenib,inhibit,PLX 4032,Inhibitor,RO-5185426,RG 7204,Raf,Autophagy,RG-7204,RO 5185426,PLX-4032 918504-65-1 API Heterocycles Intermediates & Fine Chemicals Pharmaceuticals Protein Kinase Inhibitors and Activators Sulfur & Selenium Compounds Inhibitor RG7204 Antineoplastic MAPK Inhibitors Aromatics