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PLX-4032 (Vemurafenib) | B-Raf inhibitor

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Price:
$79.00
Catalog #:
C7403-10
Quantity:


Product Description

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.


Technical information:

Chemical Formula:   C23H18ClF2N3O3S
CAS #:   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

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

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

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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Product Reviews

  1. Great customer service

    Posted by Karen on 1st May 2013

    My lab had previously used a different vendor for plx-4032. However, after buying a large batch, we had difficulty dissolving the product in DMSO at a much higher concentration than previously required, suggesting poor quality even though they promised >99%.

    When we shopped around for a different vendor, my main concern was the quality of the product, ie was the product soluble at the desired concentration. I emailed cellagentech and within a day, someone emailed me back saying they had tested the product at our desired solubility. Furthermore, they repeated the testings and were able to achieve the same results. Overall, extremely helpful and great customer service. They were able to fully answer my questions. Thank you for your help.


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