SBI-0640756

• CAT Number: I005842
• CAS Number: 1821280-29-8
• Molecular Formula: C23H14ClFN2O2
• Molecular Weight: 404.82
• Purity: ≥95%
• Synonyms: 6-chloro-3-[(E)-3-(5-fluoropyridin-3-yl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one
• InChI: InChI=1S/C23H14ClFN2O2/c24-16-7-8-19-18(11-16)21(15-4-2-1-3-5-15)22(23(29)27-19)20(28)9-6-14-10-17(25)13-26-12-14/h1-13H,(H,27,29)/b9-6+
• InChIKey: VVWGPQZBDQVQRC-RMKNXTFCSA-N
• SMILES: C1=CC=C(C=C1)C2=C(C(=O)NC3=C2C=C(C=C3)Cl)C(=O)C=CC4=CC(=CN=C4)F

SBI-0640756 (SBI-756) is an inhibitor of eIF4G1 and disrupts the eIF4F complex.
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[1].
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[1].

Reference

[1]. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex. Cancer Res, 2015 Dec 15, 75(24):5211-8.
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