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
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
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..…
N-Bromosuccinimide Price
- Product number
- orb180743
- Product name
- Vemurafenib (PLX4032)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $414.8
- Updated
- 2021/12/16
- Product number
- orb180743
- Product name
- Vemurafenib (PLX4032)
- Purity
- >98%
- Packaging
- 250mg
- Price
- $615.4
- Updated
- 2021/12/16
- Product number
- orb180743
- Product name
- Vemurafenib (PLX4032)
- Purity
- >98%
- Packaging
- 1g
- Price
- $1208.7
- Updated
- 2021/12/16
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.
brand name
Zelboraf
General Description
Class: dual threonine/tyrosine kinase; Treatment: melanoma with BRAF mutations; Elimination half-life = 57 h; Protein binding > 99%
Pharmacokinetics
1
Pharmacokinetics
The recommended daily dose of vemurafenib is
1,920 mg (4 × 240 mg tablets, BID), the highest
dosage among the three FDA-approved RAF
inhibitors (Table 2). One contributing factor for such
a high dose is the poor and variable oral
bioavailability due to both low cell permeability and
poor aqueous solubility. Nevertheless, vemurafenib
is absorbed rapidly after a single oral dose of 960 mg,
reaching a maximum drug concentration
approximately 4 h after administration. It also
exhibits long elimination half-life (57 h). It is cleared
predominantly via the hepatic route. Following oral administration, the parent drug
predominates in the plasma, and the isomeric
monohydroxylated species 5 are the only
metabolites detected in the plasma due to CYP3A4
mediated oxidation (Fig. 6).
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.
target
Primary target: BRAF
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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View Lastest Price from Plx-4032 (RG7024) manufacturers
- Product
- Vemurafenib. 1029872-54-5
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2025-01-07
- Product
- Vemurafenib 1029872-54-5
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- 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