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작성일 : 19-04-01
[Cellagen Technology LLC] PLX-4032 (Vemurafenib) | B-Raf inhibitor

 

PLX-4032 (Vemurafenib) | B-Raf inhibitor

 

 

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PLX4032 (Vemurafenib) is an 7-azaindole-based, orally-available, inhibitor of the B-Raf V600E mutation with

an IC50 of 30 nM. [1] In preclinical tumor models, PLX4032 induces antiproliferative effects in both

mealonama and thyroid cell lines, with a simultaneous dose-dependent block of MEK1/2 phosphorylation.

[1] Apoptosis is also observed in melanoma cell lines upon treatment with PLX4032. Important to note is that

proliferation was inhibited in tumor cell lines expressing B-Raf V600E only, and not B-Raf WT or other B-Raf

mutations. [2]

 

PLX4032 has marginal effect on cell-cycle arrest, apoptotic cell changes, or alteration of phosphorylated

signaling molecules in lymphocytes. T-cell function was preserved up to 10 uM of PLX4032, while cytotoxic

activty was maintained up to high concentrations of 50 uM. [3] Such observations suggest that PLX4032 can

be used in combination with immunotherapy strategies.

 

 

Details

Chemical Formula:

 

C23H18ClF2N3O3S

CAS No.:

 

1029872-54-5, 918504-65-1

Molecular Weight:

 

489.92

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-

difluorophenyl) propane-1-sulfonamide

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

PLX-4032, PLX4032, RG7204, RO5185426, Vemurafenib, Zelboraf

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

References

1.

Yang et al., RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res. 2010, 70, 5518-5527. Pubmed ID: 20551065

2.

Lee et al., PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas. Pigment Cell Melanoma Res. 2010, 23, 820-827. Pubmed ID: 20973932

3.

Comin-Anduix et al., The oncogenic BRAF kinase inhibitor PLX4032/RG7204 does not affect the viability or function of human lymphocytes across a wide range of concentrations. Cancer Res. 2010, 16, 6040-6048. Pubmed ID: 21169256

 

  

Ordering information

   

Catalog No.

Product Name

Size

C7403

PLX-4032 (Vemurafenib) | B-Raf inhibitor

10 mg, 50 mg & 250 mg

 

 

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