YUM70|cas:423145-35-1|西域试剂

YUM70,98.0%

产品编号：Bellancom-138364| CAS NO：423145-35-1| 分子式：C₂₁H₁₉ClN₂O₄| 分子量：398.84

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-138364	￥1600.00	杭州北京（现货）
Bellancom-138364	￥2500.00	杭州北京（现货）
Bellancom-138364	￥4800.00	杭州北京（现货）
Bellancom-138364	￥7200.00	杭州北京（现货）
Bellancom-138364	￥10400.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

YUM70

产品介绍

YUM70 是一种有效和选择性的葡萄糖调节蛋白 78 (GRP78) 抑制剂，抑制全长蛋白的 GRP78 ATPase 活性的 IC₅₀ 值为 1.5 μM。YUM70 可诱导内质网 (ER) 应激介导的胰腺癌细胞凋亡。YUM70 在胰腺癌异种移植模型中也具有体内功效。

生物活性

YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC₅₀ of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.

体外研究

YUM70 shows selective cytotoxicity for MIA PaCa-2, PANC-1, BxPC-3 cells (IC₅₀=2.8, 4.5, and 9.6 μM, respectively) over normal pancreatic tissue-derived HPNE cells (IC₅₀>30 μM).
YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells.

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

Western Blot Analysis

Cell Line:	MIA PaCa-2, PANC-1 cells
Concentration:	0.1, 1, 2.5, 5, 10 μM
Incubation Time:	2, 4, 8, 24, 48 hours
Result:	Increased the protein levels of FAM129A, DDIT3, CHAC-1, DDIT4, UPP1, and GRP78 in a dose- and time-dependent manner.

体内研究
(In Vivo)

YUM70 (30 mg/kg; i.p. 5 days a week for 7 weeks) inhibits tumor growth in a MIA PaCa-2 xenograft model.
YUM70 (15 mg/kg; i.v.) exhibits t_1/2 (1.40 h), CL (724.04 mL/h/kg), and V_ss (1162.73 mL/kg) in mice.
YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t_1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice.

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

Animal Model:	8-week old female NCr nude mice were injected with MIA PaCa-2 cells
Dosage:	30 mg/kg
Administration:	I.p. 5 days a week for 7 weeks
Result:	Observed a significant tumor growth delay with no significant change in body weight during the course of treatment.

体内研究

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

Animal Model:	8-week old female NCr nude mice were injected with MIA PaCa-2 cells
Dosage:	30 mg/kg
Administration:	I.p. 5 days a week for 7 weeks
Result:	Observed a significant tumor growth delay with no significant change in body weight during the course of treatment.

体内研究

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

Animal Model:	8-week old female NCr nude mice were injected with MIA PaCa-2 cells
Dosage:	30 mg/kg
Administration:	I.p. 5 days a week for 7 weeks
Result:	Observed a significant tumor growth delay with no significant change in body weight during the course of treatment.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (250.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5073 mL	12.5364 mL	25.0727 mL
5 mM	0.5015 mL	2.5073 mL	5.0145 mL
10 mM	0.2507 mL	1.2536 mL	2.5073 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: 2.5 mg/mL (6.27 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.27 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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