产品
编 号:F762444
分子式:C38H48N4O9
分子量:704.81
产品类型
结构图
CAS No: 2440087-54-5
联系客服
产品详情
生物活性:
ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors.
体内研究:
ERX-41 (10 mg/kg; 口服或腹腔注射;单次剂量) 在口服或腹腔注射后,都能够在 1.5?h 内在肿瘤内被检测到。ERX-41 (10 mg/kg; 口服; 单次剂量) 显著抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤进展而不改变小鼠体重。ERX-41 (10 mg/kg; 口服; 单次剂量) 显著抑制 D2A1 异种移植小鼠模型的疾病进展。Animal Model:Mouse models with D2A1 xenografts and MDA-MB-231 xenografts (s.c.), respectively
Dosage:10 mg/kg
Administration:Oral gavage; once daily for 25 days
Result:Reduced tumor growth against MDA-MB-231 xenograft without affecting body weight. And enhanced p-PERK and p-eIF2-α staining within 24?h.Significantly reduced the growth of D2A1 xenografts in syngeneic mice without affecting body weight.
体外研究:
ERX-41 (1 μM; 0-30 h) 诱导 MDA-MB-231 细胞死亡,对正常人乳腺上皮细胞 (HMECs) 无显著影响。ERX-41 (1 μM; 2 h, 4 h) 在 4 h 内诱导内质网急剧扩张,并在 2 h 内导致外周内质网紊乱。ERX-41 (1 μM; 0.5-4 h) 通过诱导 p-PERK 和 p-eIF2-α,诱导下游未折叠蛋白反应 (UPR) 通路。