PLX7904

SKU: orb1300319

Description

PLX7904 (PB04) is a selective paradox-breaker RAF inhibitor that suppresses ERK1/2 signaling in BRAF-mutant melanoma cells without inducing paradoxical activation in RAS-mutant contexts. Its profile supports its use in vitro and in vivo for investigating targeted therapies in oncology, particularly for overcoming resistance mechanisms in MAPK pathway-driven cancers.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1393465-84-3
• MW: 512.53
• Purity: 99.66% (May vary between batches)
• Formula: C₂₄H₂₂F₂N₆O₃S
• SMILES: CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(cc23)-c2cnc(nc2)C2CC2)c1F
• Target: Raf
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.8 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:100 mg/mL (195.11 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  B-Raf:5 nM
• In Vivo:
  PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.
• In Vitro:
  PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells. PLX7904 is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively).
• Cell Research:
  Cells are treated with PB04(PLX7904) at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

B-Raf (V600E), Inhibitor, inhibit, PB 04, PB04, PB-04, PLX7904, PLX-7904, PLX 7904, Raf, Raf kinases

Compound Identifiers

PubChem CID

90116945