产品
编 号：F354905
分子式：C21H19ClN2O4
分子量：398.84
分子式：C21H19ClN2O4
分子量：398.84
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 423145-35-1
产品详情
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.
体内研究：
YUM70 (30 mg/kg；腹腔注射，每周 5 天，持续 7 周) 抑制 MIA PaCa-2 异种移植模型中的肿瘤生长。YUM70 (15 mg/kg；静脉注射) 在小鼠中表现出 t1/2 (1.40 h)、CL (724.04 mL/h/kg) 和 Vss (1162.73 mL/kg)。 YUM70 (30 mg/kg；口服) 在小鼠中表现出低生物利用度 (6.71%)、t1/2 (2.74 h) 和 CL (9230.15 mL/h/kg)。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.
体外研究：
YUM70 对 MIA PaCa-2、PANC-1、BxPC-3 细胞表现出选择性细胞毒性 (IC50=2.8、4.5 和 9.6 μM) 超过正常胰腺组织衍生的 HPNE 细胞 (IC50>30 μM)。 YUM70 (5 μM；24 h) 诱导内质网 (ER) 应激介导的 MIA PaCa-2 细胞凋亡。
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.
体内研究：
YUM70 (30 mg/kg；腹腔注射，每周 5 天，持续 7 周) 抑制 MIA PaCa-2 异种移植模型中的肿瘤生长。YUM70 (15 mg/kg；静脉注射) 在小鼠中表现出 t1/2 (1.40 h)、CL (724.04 mL/h/kg) 和 Vss (1162.73 mL/kg)。 YUM70 (30 mg/kg；口服) 在小鼠中表现出低生物利用度 (6.71%)、t1/2 (2.74 h) 和 CL (9230.15 mL/h/kg)。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.
体外研究：
YUM70 对 MIA PaCa-2、PANC-1、BxPC-3 细胞表现出选择性细胞毒性 (IC50=2.8、4.5 和 9.6 μM) 超过正常胰腺组织衍生的 HPNE 细胞 (IC50>30 μM)。 YUM70 (5 μM；24 h) 诱导内质网 (ER) 应激介导的 MIA PaCa-2 细胞凋亡。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备