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 ofglucose-regulated protein 78 (GRP78), with anIC50of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediatedapoptosisin pancreaticcancer. YUM70 also has in vivo efficacy in a pancreaticcancerxenograft 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].
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. |
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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].
| 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. |
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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 : 100 mg/mL(250.73 mM;Need ultrasonic) 配制储备液 | 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 |
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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: 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。 *以上所有助溶剂都可在本网站选购。
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