Lifirafenib

SKU: orb1218803

Description

Lifirafenib is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively.

Key Properties

• CAS Number: 1446090-79-4
• MW: 478.42
• Purity: >98% (HPLC)
• Formula: C₂₅H₁₇F₃N₄O₃
• SMILES: O=C1Nc2nccc(Oc(cc3)cc(C45)c3OC4C5c3nc(ccc(C(F)(F)F)c4)c4[nH]3)c2CC1
• Target: EGFR
• Solubility: DMSO:100 mg/mL (209.02 mM)

Bioactivity

• In Vivo:
  Lifirafenib (BGB-283) treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRafV600E mutation.
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• In Vitro:
  Lifirafenib (BGB-283) potently inhibits BRafV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Beigene-283 | BGB-283

Quick Database Links

Gene Symbol

EGFR