YUM70 |
| رقم الكتالوجGC62388 |
YUM70 هو مثبط قوي وانتقائي للبروتين 78 المنظم للجلوكوز (GRP78) ، مع IC 50 من 1.5 ميكرومتر لتثبيط نشاط GRP78 ATPase للبروتين كامل الطوليستحث YUM70 الشبكة الإندوبلازمية (ER) بوساطة الإجهاد في سرطان البنكرياسلدى YUM70 أيضًا فعالية في الجسم الحي في نموذج طعم أجنبي لسرطان البنكرياس
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 423145-35-1
Sample solution is provided at 25 µL, 10mM.
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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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