ChemicalBook > CAS DataBase List > Plx-4032 (RG7024)

Plx-4032 (RG7024)

Product Name
Plx-4032 (RG7024)
CAS No.
1029872-54-5
Chemical Name
Plx-4032 (RG7024)
Synonyms
vemurafenib;Zelboraf;RG 7204;RO 5185426;Plx-4032 (RG7024);Vemurafenib, >=98%;VeMurafenib,PLX 4032;Plx-4032 (RG7024) USP/EP/BP;PLX 4032; RG 7204; RO 5185426;Vemurafenib Plx-4032 (RG7024)
CBNumber
CB22515128
Molecular Formula
C23H18ClF2N3O3S
Formula Weight
489.9221264
MOL File
1029872-54-5.mol
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Plx-4032 (RG7024) Property

Melting point:
>263oC (dec.)
storage temp. 
Refrigerator
solubility 
DMSO (Slightly, Heated), Methanol (Slightly, Heated)
form 
Solid
color 
Off-White
CAS DataBase Reference
1029872-54-5
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H350May cause cancer

H361Suspected of damaging fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P281Use personal protective equipment as required.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Biorbyt Ltd
Product number
orb180743
Product name
Vemurafenib (PLX4032)
Purity
>98%
Packaging
100mg
Price
$414.8
Updated
2021/12/16
Biorbyt Ltd
Product number
orb180743
Product name
Vemurafenib (PLX4032)
Purity
>98%
Packaging
250mg
Price
$615.4
Updated
2021/12/16
Biorbyt Ltd
Product number
orb180743
Product name
Vemurafenib (PLX4032)
Purity
>98%
Packaging
1g
Price
$1208.7
Updated
2021/12/16
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Plx-4032 (RG7024) Chemical Properties,Usage,Production

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. Potent B-Raf inhibitor

Definition

ChEBI: Vemurafenib is 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 formal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases. It has a role as an antineoplastic agent and a B-Raf inhibitor. It is a pyrrolopyridine, a sulfonamide, a member of monochlorobenzenes, a difluorobenzene and an aromatic ketone.

Clinical Use

Vemurafenib was originally discovered at Plexxikon and has been co-developed by Roche and Plexxikon as an oral BRAF inhibitor for the treatment of patients with BRAFV600E mutation- positive metastatic melanoma. The drug displays good potency and selectivity for the V600E mutation (IC50 = 3.2–14 nM), an oncoprotein, over the wild-type BRAF (IC50 = 21–370 nM). The compound is less potent in in vitro kinase assays than other Plexxikon BRAF inhibitors, but it was selected for clinical development based on its enhanced potency against the BARFV600E-containing A374 melanoma cell line.

Synthesis

The synthesis described below is based on a recent process patent (the Scheme).


Commercially available 2-amino-5-bromopyridine (271) was treated with 4-chlorophenylboronic acid (272) in the presence of Na2CO3 and a catalytic amount of Pd(OAc)2/PdCl2(dppf)CH2Cl2 to give Suzuki product 273 in 83% yield. Arene 273 was subjected to iodination conditions using NIS and TFA to provide iodide 274 in 98% yield. Iodide 274 and pinacol vinylboronate 275 were coupled under Suzuki conditions followed by treatment with acid to affect a tandem coupling¨Ccyclization sequence which resulted in pyrimidyl pyrrole 276 in good yield. This material was treated with aluminum trichloride and then subjected to the the acyl chloride of commercially available sulfonamide acid 277, triggering a Friedel- Crafts reaction providing vemurafenib (XXIV) in 85% yield.

Drug interactions

Potentially hazardous interactions with other drugs
Anticoagulants: possibly enhances anticoagulant effect of warfarin.
Antipsychotics: avoid concomitant use with clozapine, risk of agranulocytosis.
Oestrogens and progestogens: contraceptive effect possibly reduced.

Metabolism

Only 5
% of a dose of vemurafenib is metabolised. 94
% of the dose is excreted in the faeces and 1
% in the urine.

Plx-4032 (RG7024) Preparation Products And Raw materials

Raw materials

Preparation Products

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Plx-4032 (RG7024) Suppliers

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2923
Advantage
55
ZHIWE CHEMTECH CO LTD
Tel
021-20221225 13917446399
Fax
QQ:115820162
Email
sales@zhiwe.net
Country
China
ProdList
579
Advantage
61
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9984
Advantage
60
China DongFan Chemical Co.,LTD
Tel
86-0571-85151182
Fax
86-0571-85151182
Country
China
ProdList
5700
Advantage
66
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com (International market)
Country
China
ProdList
1856
Advantage
62
Shanghai Sunway Pharmaceutical Technology Co., Ltd
Tel
13761588971 13761588971
Fax
021 51613951
Email
vivian.zhu@3wpharm.com
Country
China
ProdList
9840
Advantage
57
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-83725681-603
Fax
+86 755 28094224
Country
China
ProdList
4505
Advantage
50
Beijing HuaMeiHuLiBiological Chemical
Tel
010-56205725
Fax
010-65763397
Email
waley188@sohu.com
Country
China
ProdList
12338
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1494
Advantage
55
Nanjing Norris-Pharm Technology Co., Ltd
Tel
13901585132
Fax
+86-25-52131256
Email
799750417@qq.com
Country
China
ProdList
8888
Advantage
55
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View Lastest Price from Plx-4032 (RG7024) manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Plx-4032 (RG7024) 1029872-54-5
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-06-26
Dideu Industries Group Limited
Product
Plx-4032 (RG7024) 1029872-54-5
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons Min
Release date
2021-06-30
Shaanxi Dideu Medichem Co. Ltd
Product
Vemurafenib 1029872-54-5
Price
US $0.00-0.00/Kg
Min. Order
1KG
Purity
99.0%+
Supply Ability
800 tons
Release date
2020-04-29

1029872-54-5, Plx-4032 (RG7024)Related Search:


  • Plx-4032 (RG7024)
  • PLX 4032; RG 7204; RO 5185426
  • RG 7204
  • RO 5185426
  • vemurafenib
  • N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-PropanesulfonaMide
  • N-(3-{[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonaMide
  • VeMurafenib,PLX 4032
  • Zelboraf
  • 1-PropanesulfonaMide, N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-
  • Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
  • Vemurafenib, >=98%
  • Vemurafenib Plx-4032 (RG7024)
  • PLX4032,Vemurafenib, Free Base
  • (1R)-1-(4-Hydroxy-3-{[(1R)-6-methoxy-1-(4-methoxybenzyl)-2-methyl -1,2,3,4-tetrahydro-7-isoquinolinyl]oxy}benzyl)-6-methoxy-2-methy l-1,2,3,4-tetrahydro-7-isoquinolinol
  • Plx-4032 (RG7024) USP/EP/BP
  • -(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide
  • 1029872-54-5
  • C23H18ClF2N3O3S