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SBI-0640756

SBI-0640756 is an inhibitor of eIF4G1 which can disrupt the function of eIF4F complex.

CAS号

2205871-61-8

分子式

C23H14ClFN2O2

主要靶点

eIF

仅限科研使用

Cat No : CM03935

Print datasheet

Synonyms

SBI-756

验证数据展示

  • CAS No.: 2205871-61-8

    SBI-0640756
    CAS#: 2205871-61-8

  • SBI-0640756<br/>CAS#: 2205871-61-8

    SBI-0640756
    CAS#: 2205871-61-8

产品信息

The Eukaryotic Translation Initiation Factor 4 Gamma 1(eIF4G1) is a large scaffolding protein that is a key component of the eIF4F complex, it serves as a scaffold for assembly of cap-dependent translation components in EIF4F complex formation[1]. Elevated eIF4F activity has been linked to resistance to BRAF- and MEK targeted therapies[2]. SBI-0640756 (SBI-756), which retained the biological effects of the original compound while possessing superior pharmacokinetics. Extended characterization of SBI-756 identified eIF4G1 as its direct target[3]. SBI-756 impaired the eIF4F complex assembly independently of mTOR and attenuated growth of BRAF-resistant and BRAF-independent melanomas. SBI-756 also suppressed AKT and NF-κB signaling, but small-molecule derivatives were identified that only marginally affected these pathways while still inhibiting eIF4F complex formation and melanoma growth[4]. Treatment of DLBCL and MCL cells with SBI-756 synergised with venetoclax to induce apoptosis in vitro, and enhanced venetoclax efficacy in vivo. SBI-756 prevented eIF4E-eIF4G1 association and cap-dependent translation without affecting mTOR substrate phosphorylation. In TOR-KI-resistant DLBCL cells lacking eIF4E binding protein-1, SBI-756 still sensitised to venetoclax. SBI-756 selectively reduced translation of mRNAs encoding ribosomal proteins and translation factors, leading to a reduction in protein synthesis rates in sensitive cells. When normal lymphocytes were treated with SBI-756, only B cells had reduced viability, and this correlated with reduced protein synthesis[5].

CAS号 2205871-61-8
分子式 C23H14ClFN2O2
主要靶点 eIF
主要通路 Cell Cycle
分子量 404.8209
MDL NO
Pubchem ID 121241171.0
纯度 99.86%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件
粉末 -20°C 3年
液体 -80°C 1年
运输条件 Shipped in cold pack
别名 SBI-756

溶解度

DMSO235 mg/mL
Waterinsoluble

参考文献

1Praveen Kumar Jaiswal,et al. Eukaryotic Translation Initiation Factor 4 Gamma 1 (EIF4G1): a target for cancer therapeutic intervention? Cancer Cell Int. 2019 Aug 31;19:224.
2Sonenberg N, Hinnebusch AG. Regulation of translation initiation in eukaryotes: mechanisms and biological targets. Cell. 2009; 136(4):731–45.
3Boussemart L, Malka-Mahieu H, Girault I, Allard D, Hemmingsson O, Tomasic G, et al. eIF4F is a nexus of resistance to anti-BRAF and anti-MEK cancer therapies. Nature. 2014; 513(7516):105–9.
4Yongmei Feng,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.
5Lee-Or Herzog,et al. Targeting eIF4F translation initiation complex with SBI-756 sensitises B lymphoma cells to venetoclax. Br J Cancer. 2021 Mar;124(6):1098-1109.

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