|(E)-6-氯-3-(3-(5-氟吡啶-3-基)丙烯酰基)-4-苯基喹啉-2(1H)-酮|CsnPharm

CAS No.: 2205871-61-8

(E)-6-Chloro-3-(3-(5-fluoropyridin-3-yl)acryloyl)-4-phenylquinolin-2(1H)-one Catalog No. CSN23286

Synonyms: SBI-0640756

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

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实验方案

技术信息

生物活性

描述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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4702 mL
- 12.3511 mL
- 24.7023 mL
- 5 mM
- 0.4940 mL
- 2.4702 mL
- 4.9405 mL
- 10 mM
- 0.2470 mL
- 1.2351 mL
- 2.4702 mL

技术信息

CAS号

2205871-61-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H14ClFN2O2

运输

蓝冰

分子量

404.82

别名

SBI-0640756

溶解度

DMSO	235.0 mg/mL (580.5 mM)
Water	insoluble

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(E)-6-Chloro-3-(3-(5-fluoropyridin-3-yl)acryloyl)-4-phenylquinolin-2(1H)-one Catalog No. CSN23286

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