规格 | 5 mg 10 mg 25 mg |
CAS | 423145-35-1 |
别名 | N/A |
化学名 | N/A |
分子式 | C21H19ClN2O4 |
分子量 | 398.84 |
溶解度 | DMSO : 100 mg/mL (250.73 mM; Need ultrasonic) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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[1].
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].
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].
[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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