Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SBI-0640756 (SBI-756) 是一种靶向 eIF4G1 并破坏 eIF4F 复合物的抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 398 | 现货 | ||
2 mg | ¥ 578 | 现货 | ||
5 mg | ¥ 1,110 | 现货 | ||
10 mg | ¥ 1,780 | 现货 | ||
25 mg | ¥ 3,330 | 现货 | ||
50 mg | ¥ 4,760 | 现货 | ||
100 mg | ¥ 6,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,210 | 现货 |
产品描述 | SBI-0640756 (SBI-756) (SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex. |
体外活性 | SBI-756 effectively dissociated eIF4G1 from the eIF4E in a dose-dependent manner, which was accompanied by a concomitant increase in 4E-BP1:eIF4E binding, reflective of impaired eIF4F complex formation. SBI-756 also inhibits the AKT/mTORC1 signaling and mTORC1 inhibition disrupts the eIF4F complex via activation of 4E-BPs. Whereas torin1 induced dissociation of eIF4G1 from eIF4E in WT but not in 4E-BP DKO MEFs, SBI-756 reduced eIF4G1:eIF4E association in both WT and 4E-BP DKO MEFs. Likewise, SBI-756 but not torin1 attenuated the proliferation of E1A/RAS-transformed 4E-BP DKO MEFs. |
体内活性 | Administration of SBI-756 only, starting 11 weeks after genetic inactivation of Ink4a and induction of NRasQ61E (about 10–14 days prior to tumor appearance), delayed tumor onset (from 20–26 weeks) and reduced tumor incidence, by 50%, compared with the control non-treated group. The growth of established tumors was largely inhibited by treatment with either BRAFi alone or a combination of BRAFi plus SBI-756. |
细胞实验 | Cells were rinsed with PBS and lysed as previously described. Protein concentration was determined using Coomassie Plus Protein Assay Reagent. Equal amounts of cell lysate proteins (50 μg) were separated on SDS-PAGE and transferred to polyvinylidene difluoride membranes. Membranes were blocked (5% BSA/TBST, 1 h) and incubated with primary antibodies (1 h at room temperate or overnight at 4°C), with shaking. Following three TBST washes, membranes were incubated for 1 h at room temperature secondary antibodies (1:10,000). Detection and quantifications were made using Odyssey Infrared Imaging System, or by exposing them to X-ray film. Antibodies against p-AKT, p-PRAS40, p-IKK, p-IκB, p-TSC, p-mTOR, p-p70S6K, p-RPS6, p-4E-BP1, pSGK3, AKT, PRAS40, IKK, IκB, mTOR, p70S6K, RPS6, 4E-BP1, GSK3, eIF4G1, and eIF4E were purchased from Cell Signaling Technology. Antibodies against β-actin and α-tubulin were obtained from Santa Cruz Biotechnology. Secondary antibodies were goat anti-rabbit Alexa-680 F(ab')2 and goat anti-mouse IRDye 800 F(ab')2. All antibodies were used according to the suppliers' recommendations. |
别名 | SBI 0640756, SBI-756 |
分子量 | 404.82 |
分子式 | C23H14ClFN2O2 |
CAS No. | 1821280-29-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 50 mg/mL (123.51 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4702 mL | 12.3512 mL | 24.7023 mL | 61.7558 mL |
5 mM | 0.494 mL | 2.4702 mL | 4.9405 mL | 12.3512 mL | |
10 mM | 0.247 mL | 1.2351 mL | 2.4702 mL | 6.1756 mL | |
20 mM | 0.1235 mL | 0.6176 mL | 1.2351 mL | 3.0878 mL | |
50 mM | 0.0494 mL | 0.247 mL | 0.494 mL | 1.2351 mL | |
100 mM | 0.0247 mL | 0.1235 mL | 0.247 mL | 0.6176 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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