• 产品描述： 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

• 靶点： IC50: 1.5 μM (glucose-regulated protein 78);Apoptosis; GPR; HSP

• 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. 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：
  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 t1/2 (1.40 h), CL (724.04 mL/h/kg), and Vss (1162.73 mL/kg) in mice. YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice. 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.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.507 ml	12.536 ml	25.073 ml
  5 mM	0.501 ml	2.507 ml	5.015 ml
  10 mM	0.251 ml	1.254 ml	2.507 ml
  50 mM	0.05 ml	0.251 ml	0.501 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *