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PLX4032

PLX4032 Structure
PLX4032
  • CAS No.918504-65-1
  • Chemical Name:PLX4032
  • CBNumber:CB02550000
  • Molecular Formula:C23H18ClF2N3O3S
  • Formula Weight:489.92
  • MOL File:918504-65-1.mol
PLX4032 Property
  • 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
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H410
  • Precautionary statements P273-P391-P501

PLX4032 Chemical Properties,Usage,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
PLX4032 Suppliers
Global(259)Suppliers
  • Supplier：
    Henan Tianfu Chemical Co.,Ltd.
  • Tel：+86-0371-55170693<br/>+86-19937530512
  • Email：info@tianfuchem.com
  • Country：China
  • ProdList：21628
  • Advantage：55
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：sales@coreychem.com
  • Country：China
  • ProdList：29858
  • Advantage：58
  • Supplier：
    BOC Sciences
  • Tel：+1-631-485-4226
  • Email：inquiry@bocsci.com
  • Country：United States
  • ProdList：19552
  • Advantage：58
  • Supplier：
    Alchem Pharmtech,Inc.
  • Tel：8485655694
  • Email：sales@alchempharmtech.com
  • Country：United States
  • ProdList：63687
  • Advantage：58
PLX4032 Spectrum
918504-65-1, PLX4032Related Search:
  • Aromatics
  • Inhibitors
  • MAPK
  • Antineoplastic
  • RG7204
  • Inhibitor
  • Sulfur & Selenium Compounds
  • Protein Kinase Inhibitors and Activators
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Heterocycles
  • API
  • 抑制剂
  • 化工试剂
  • 药靶配体
  • FDA批准的配体
  • 普通产品
  • 原料
  • 有机化学
  • 小分子抑制剂，天然产物
  • 抗肿瘤原料药
  • 化学试剂
  • 小分子抑制剂
  • 抗肿瘤类药物及免疫抑制剂
  • 威罗菲尼-[13C6]/精确称量
  • 维罗非尼 6级
  • 13C6]-维罗非尼
  • N-(3-(5-(4-氯苯基)-1H-吡咯并[2,3-B]吡啶-3-羰基)-2,4-二氟苯基)丙烷-1-磺酰胺
  • 威罗非尼
  • 维罗非尼/N-(3-(5-(4-CHLOROPHENYL)-1H-PYRROLO[2,3-B]PYRIDINE-3-CARBONYL)-2,4-DIFLUOROPHENYL)PROPANE-1-SULFONAMIDE
  • 唯罗非尼
  • 维罗非尼 1G
  • 维罗非尼(PLX4032, RG7204)
  • 维罗非尼,RG7204
  • 维罗菲尼
  • 维罗非尼,VEMURAFENIB
  • 威罗菲尼
  • 918504-65-1
  • Raf kinases,Vemurafenib,inhibit,PLX 4032,Inhibitor,RO-5185426,RG 7204,Raf,Autophagy,RG-7204,RO 5185426,PLX-4032
  • 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
  • Vemurafenib (10mM in DMSO)
  • N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide USP/EP/BP
  • (1029872-54-5) vemurafenib
  • 104532
  • PLX 4032 - RG 7204 | Vemurafenib | RO 5185426
  • CS-1916
  • RG7204;PLX-4032;PLX 4032;RG-7204
  • Vemurafenib (RG7204,PLX4032)
  • Vemurafenib, >=99%
  • Zelboraf (vemurafenib)
  • N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide Vemurafenib PLX 4032
  • VeMurafenib (PLX4032, RG7204)
  • PLX4032, R7204, RG7204, RO5185426
  • N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaM
  • R7204
  • PLX4032, RG7204, ZELBORAF, RO5185426
  • PLX4032 (VeMurafenib)
  • N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide

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