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PLX4032

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:2023-06-30 15:45:59

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)  GHS hazard pictograms
GHS09
Signal word  Warning
Hazard statements  H410
Precautionary statements  P273-P391-P501
HS Code  29339900

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 IC50's of <100 nM.

Chemical Properties

Off-White Solid

Originator

Plexxikon (United States)

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]

Uses

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM

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.

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

Global( 247)Suppliers
Supplier Tel Email Country ProdList Advantage
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21703 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Shandonghaohong biotechnology Co.,ltd.
0635-6175299 13961496334 sale@inyelchem.com CHINA 44 55
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29919 58
Shanghai Arbor Chemical Co., Ltd.
021-60451682 act@arborchemical.com CHINA 906 58
Accela ChemBio Inc.
(+1)-858-699-3322 info@accelachem.com United States 19965 58
Hubei xin bonus chemical co. LTD
86-13657291602 linda@hubeijusheng.com CHINA 22968 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Alchem Pharmtech,Inc.
8485655694 sales@alchempharmtech.com United States 63711 58

View Lastest Price from PLX4032 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Vemurafenib pictures 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
Vemurafenib pictures 2021-07-10 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 USP/EP/BP pictures 2021-07-02 N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide USP/EP/BP
918504-65-1
US $1.10 / g 1g 99.9% 100 Tons Min Dideu Industries Group Limited
  • Vemurafenib pictures
  • Vemurafenib
    918504-65-1
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd
  • Vemurafenib pictures
  • Vemurafenib
    918504-65-1
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

PLX4032 Spectrum

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