CR-1-31-B|cas:1352914-52-3|西域试剂

CR-1-31-B,98.36%

产品编号：Bellancom-136453| CAS NO：1352914-52-3| 分子式：C₂₈H₂₉NO₈| 分子量：507.53

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货号	价格	库存与货期
Bellancom-136453	￥8500.00	杭州北京（现货）
Bellancom-136453	￥14500.00	杭州北京（现货）
Bellancom-136453	￥28500.00	杭州北京（现货）

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CR-1-31-B

产品介绍

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 potent eIF4A inhibitor. 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 of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells^[4].

体外研究

CR-1-31-B (100 nM; 24 hours) inhibits MUC1-C translation in MCF-10A cells (EGF-stimulated).
CR-1-31-B (10 and 100 nM) decreases MUC1-C abundance in MDA-MB-468 breast cancer cells.
CR-1-31B sensitizes gallbladder cancer cells to TRAIL-mediated apoptosis through the translational downregulation of c-FLIP.
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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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 IC₅₀ at 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.

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).
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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 230 mg/mL (453.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。