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
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 |
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 |
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21668 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 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 | 29894 | 58 |
Shanghai Arbor Chemical Co., Ltd. | 021-60451682 | act@arborchemical.com | CHINA | 906 | 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 | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39916 | 58 |
Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63711 | 58 |
Shenzhen Excellent Biotech Co., Ltd. | 13480692018 | ramyan@ex-biotech.com | CHINA | 954 | 58 |
View Lastest Price from PLX4032 manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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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 | |
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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 | |
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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
918504-65-1
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
-
- Vemurafenib
918504-65-1
- US $15.00-10.00 / KG
- 99%+ HPLC
- 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
918504-65-1
- US $1.10 / g
- 99.9%
- Dideu Industries Group Limited