Cellagentech/PLX-4720 | B-RAF inhibitor/C7420-5/5 mg (powder)
Product Description
PLX-4720 is an orally-available, ATP-competitive, highly selective, azaindole-based inhibitor of B-Raf (V600E) with IC50 value of 13 nM. PLX-4720 has additional activity towards mutant forms of c-Raf-1 (Y340D, Y341D) at an IC50 of 6.7 nM, with modest single micromolar activity versus kinases such as FRK, CSK, SRC, FGFR, KDR< HGK, and Aurora A. [1] PLX-4720 has shown preclinical activity in melanoma and thyroid cancer models. [1, 2]PLX-4720 preferentiallly inhibits ERK phosphorylation in tumor cell lines bearing the V600E allele. In melanoma models it induces cell cycle arrest and apoptosis exclusively in B-Raf (V600E)-positive cells.In an orthotopic 8505c human thyroid cancer mice model, PLX-4720 caused significant reduction in tumor growth (>90%) and dramatically decreased lung metastases. [3]
Technical information:
| Chemical Formula: | C17H14ClF2N3O3S | |
| CAS #: | 918505-84-7 | |
| Molecular Weight: | 413.83 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | N-(3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | PLX-4720, PLX4720 |
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. | Tsai et al., Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc. Natl. Acad. Sci. 2008, 105(8), 3041-3046. Pubmed ID: 18287029 |
| 2. | Nucera et al., Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. The Oncologist, 2011, 16, 296-309. Pubmed ID: 21355020 |
| 3. | Nucera et al., B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression. Proc. Natl. Acad. Sci. 2010, 107(23), 10649-10654. Pubmed ID: 20498063 |
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