Belvarafenib

SKU: orb1226265

Description

Belvarafenib (HM95573, GDC5573) is a novel potent, selective RAF inhibitor with IC50 of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF V600E and CRAF, respectively; inhibits cell proliferation of A375 (BRAF V600E) and SK-MEL-30 (NRAS Q61K) with IC50 of 57 and 24 nM, also inhibits the phosphorylations of MEK and ERK downstream kinases in mutant BRAF and mutant NRAS melanoma cells; shows the excellent antitumor activity in mouse models xenografted with both of BRAF mutation cell lines (e.g. A375 and SK-MEL-28) and NRAS mutation cell lines.(In Vitro):Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively.

Key Properties

• CAS Number: 1446113-23-0
• MW: 478.93
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₆ClFN₆OS
• SMILES: FC1=C(Cl)C=CC=C1NC2=NC=CC3C(NC(C4=CSC5=C4N=CN=C5N)=O)=CC(C)=CC23
• Target: Raf
• Solubility: In Vitro: DMSO : 12.5 mg/mL (26.10 mM)

Bioactivity

• In Vitro:
  Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively.
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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

HM95573 | GDC5573

Quick Database Links

Gene Symbol

Raf