PLX4720
PLX4720 is an orally available ATP-competitive kinase inhibitor specific for mutant (V600E) B-Raf, which is present in a variety of cancer subtypes. PLX4720 is an analog of vemurafenib. This compound is being examined as a treatment for unresectable or metastatic melanomas. Inhibition of B-Raf by PLX4720 induces apoptosis and autophagy in tumor cells, resulting in decreased tumor growth and increased survival in vitro and in vivo. Additional downstream effects of B-Raf inhibition by PLX4720 include downregulation of expression of angiogenic factors, enhancement of surface expression of tumor-associated antigens on tumor cells, and alterations of trafficking of local immune cells such as CD8+ T lymphocytes.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18955292
| Cas No. |
918505-84-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C17H14ClF2N3O3S |
| Formula Wt. |
413.83 |
| IUPAC Name |
N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide |
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Bottos A, Martini M, Di Nicolantonio F, et al. Targeting oncogenic serine/threonine-protein kinase BRAF in cancer cells inhibits angiogenesis and abrogates hypoxia. Proc Natl Acad Sci U S A. 2012 Feb 7;109(6):E353-9. PMID: 22203991.
Wilmott JS, Long GV, Howle JR, et al. Selective BRAF inhibitors induce marked T-cell infiltration into human metastatic melanoma. Clin Cancer Res. 2012 Mar 1;18(5):1386-94. PMID: 22156613.
Boni A, Cogdill AP, Dang P, et al. Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function. Cancer Res. 2010 Jul 1;70(13):5213-9. PMID: 20551059.
