PLX-4720

PLX-4720

Catalog Number:
L002368475APE
Mfr. No.:
APE-A3016
Price:
$220
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      • Overview
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          Background

          PLX-4720, a 7-azaindole derivative discovered by a structure-guided discovery approach, is a potent inhibitor of B-RafV600E, the most frequent oncogenic protein kinase mutation, with the value of 50% inhibition concentration IC50 of 13 nM. PLX-4720 exhibits selective inhibition against B-RafV600E rather than wild type B-Raf (IC50 = 160 nM) as well as a wide range of other kinases, such as FRK, CSK, SRC, FAK, FGFR, and Aurora A (IC50 > 1000 nM for all). PLX-4720 potently inhibits ERK phosphorylation in tumor cell lines harboring B-RafV600E, induces cell cycle arrest and apoptosis in B-RafV600E-positive melanoma cells and causes tumor growth delays in B-RafV600E-dependent tumor xenograft models through oral administration.

      • Properties
        • Alternative Name
          PLX4720, PLX-4720, PLX 4720; N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide
          CAS Number
          918505-84-7
          Molecular Formula
          C17H14ClF2N3O3S
          Molecular Weight
          413.83
          Appearance
          A solid
          Purity
          98.70%
          Solubility
          ≥20.69 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at 4°C

          * For Research Use Only

      • Reference
        • 1. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695

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