YUM70

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YUM70  纯度: ≥98.0%

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。

YUM70

YUM70 Chemical Structure

CAS No. : 423145-35-1

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
25 mg ￥11000 In-stock
50 mg 询价
100 mg 询价

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YUM70 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library

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[1].

IC50 & Target

IC50: 1.5 μM (glucose-regulated protein 78)[1]
体外研究
(In Vitro)

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)[1].
YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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[1].
YUM70 (15 mg/kg; i.v.) exhibits t1/2 (1.40 h), CL (724.04 mL/h/kg), and Vss (1162.73 mL/kg) in mice[1].
YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice[1].

上海金畔生物科技有限公司 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[1]
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.

分子量

398.84

Formula

C21H19ClN2O4
CAS 号

423145-35-1
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 : 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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Samanta S, et, al. The hydroxyquinoline analog YUM70 inhibits GRP78 to induce ER stress-mediated apoptosis in pancreatic cancer. Cancer Res. 2021 Feb 2;canres.1540.2020.

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