CR-1-31-B 是一种合成的 Rocaglate 和一种有效的eIF4A抑制剂。CR-1-31-B 通过干扰 eIF4A 和 RNA 之间的相互作用，依次阻碍蛋白质合成过程中的起始，从而对 eIF4A 表现出强大的抑制作用。CR-1-31-B 扰乱恶性疟原虫 eIF4A (PfeIF4A) 与 RNA 的关联。CR-1-31-B 导致神经母细胞瘤和胆囊癌细胞凋亡。
| 生物活性 | CR-1-31-B is a synthetic rocaglate and a potenteIF4Ainhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association ofPlasmodiumfalciparumeIF4A (PfeIF4A) with RNA. CR-1-31-B inducesapoptosisof neuroblastoma and gallbladdercancercells[1][2][3][4]. |
体外研究
(In Vitro) | CR-1-31-B (100 nM; 24 hours) inhibits MUC1-C translation in MCF-10A cells (EGF-stimulated)[1].
CR-1-31-B (10 and 100 nM) decreases MUC1-C abundance in MDA-MB-468 breast cancer cells[1].
CR-1-31B sensitizes gallbladder cancer cells to TRAIL-mediated apoptosis through the translational downregulation of c-FLIP[2].
Neuroblastoma (NB) cell lines exhibit decreased viability, increased apoptosis rates as well as changes in cell cycle distribution when treated with the synthetic rocaglate CR-1-31-B (24-72 hours), which clamps eIF4A and eIF4F onto mRNA, resulting in a translational block[4].
CR-1-31-B (100 nM; 5 hours) treatment increases reverse glutamine metabolism in pancreatic cancer cells[5].
Western Blot Analysis[1] | Cell Line: | MCF-10A cells (EGF-stimulated) | | Concentration: | 100 nM | | Incubation Time: | 24 hours | | Result: | Blocked increases in MUC1-C abundance. |
Cell Viability Assay[4] | Cell Line: | SH-SY5Y cells and Kelly cells | | Concentration: | 0.1-100 nM | | Incubation Time: | 24-72 hours | | Result: | A significant decrease in SH-SY5Y viability was observed at 10 nM for all time points. Significantly decreased the viability of Kelly cells at 5 nM. The calculated IC50at 48 h was 20 nM for SH-SY5Y and 4 nM for Kelly cells. |
Apoptosis Analysis[4] | Cell Line: | SH-SY5Y and Kelly cells | | Concentration: | SH-SY5Y cells were treated with 10, 20, and 50 nM and Kelly cells with 1, 5, and 10 nM | | Incubation Time: | 24-72 hours | | Result: | Triggered apoptosis. |
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体内研究
(In Vivo) | CR-1-31-B (2 mg/kg in 60 μL olive oil; IP; once every 2 days for 28 days) reduces the growth and initiates TRAIL-induced apoptosis in a BALB/c nude mice model of gallbladder cancer cells (GBC)[2].
CR-1-31-B (0.2 mg/kg; IP; daily for 7 days; murine orthotopic transplant model of pancreatic ductal adenocarcinoma) effectively inhibits protein synthesis and growth of pancreatic tumours[5].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 230 mg/mL(453.18 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9703 mL | 9.8516 mL | 19.7033 mL | | 5 mM | 0.3941 mL | 1.9703 mL | 3.9407 mL | | 10 mM | 0.1970 mL | 0.9852 mL | 1.9703 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5.75 mg/mL (11.33 mM); Clear solution
此方案可获得 ≥ 5.75 mg/mL (11.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5.75 mg/mL (11.33 mM); Clear solution
此方案可获得 ≥ 5.75 mg/mL (11.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5.75 mg/mL (11.33 mM); Clear solution
此方案可获得 ≥ 5.75 mg/mL (11.33 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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