CR-1-31-B - CAS:1352914-52-3

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CR-1-31-B

目录号 : KM10700 CAS No. : 1352914-52-3 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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.

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.
CR-1-31-B (100 nM; 5 hours) treatment increases reverse glutamine metabolism in pancreatic cancer cells.

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

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

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

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.

分子式

C₂₈H₂₉NO₈

分子量

507.53

CAS号

1352914-52-3

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

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。
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。
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。