SBI-0640756

SKU: orb1225872

Description

SBI-0640756 (SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex; impairs the eIF4F complex assembly and attenuates growth of BRAF-resistant and BRAF-independent melanomas; inhibits the growth of NRAS, BRAF, and NF1-mutant melanomas in vitro, delays the onset and reduces the incidence of Nras/Ink4a melanomas in vivo; attenuates the formation of BRAFi-resistant human tumors combined with PLX4720 in vivo.

Key Properties

• CAS Number: 1821280-29-8
• MW: 404.8209
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₄ClFN₂O₂
• SMILES: O=C1NC2=C(C=C(Cl)C=C2)C(C3=CC=CC=C3)=C1C(/C=C/C4=CC(F)=CN=C4)=O
• Target: eIF
• Solubility: DMSO: ≥ 26 mg/mL

Bioactivity

• In Vivo:
  SBI-0640756 (SBI-756) (0.5 mg/kg, i.p.) delays tumor onset and reduces tumor incidence by 50% in NrasQ61K/Ink4a–/– genetic model. SBI-0640756 (SBI-756) (1 mg/kg, 2 times per week, i.p.) in combination with BRAF inhibitor potently suppresses growth of established tumors and does not resume tumor growth in immunodeficient mice bearing A375 tumors.
• In Vitro:
  SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1. SBI-0640756 (SBI-756) (0-1 μM) disrupts eIF4F complex in parent and BRAFi-resistant melanoma. SBI-0640756 (SBI-756) shows inhibitory effect on human melanoma lines, and also suppresses AKT, NF-κB and AKT/mTORC1 activity.

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

SBI-756

Quick Database Links

Gene Symbol

eIF