SBI-0640756

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SBI-0640756 (SBI-756) 是一种针对 eIF4G1 并破坏 eIF4F 复合物的一流抑制剂。

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.

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.

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.

SBI-756

Nuclear Receptor/Transcription Factor

eIF

eIF4G1

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1821280-29-8

404.8209

C23H14ClFN2O2

>98% (HPLC)

DMSO: ≥ 26 mg/mL

O=C1NC2=C(C=C(Cl)C=C2)C(C3=CC=CC=C3)=C1C(/C=C/C4=CC(F)=CN=C4)=O

(E)-6-chloro-3-(3-(5-fluoropyridin-3-yl)acryloyl)-4-phenylquinolin-2(1H)-one

(-20℃)

With Ice Pack

≥ 2 years