产品
编 号:F580368
分子式:C19H15N3O5
分子量:365.34
产品类型
结构图
CAS No: 919091-63-7
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生物活性:
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
体内研究:
RA-9 (5 mg/kg;腹腔注射;服用一天,停药两天) 在卵巢癌小鼠模型中抑制体内人卵巢癌细胞生长并延长存活期。Animal Model:Six-week-old female immunodeficient (NCr nu/nu) mice
Dosage:5 mg/kg
Administration:I.p; one-day on, two-days off
Result:Significant reduction in tumor burden at day 12.
体外研究:
RA-9 (10-30 μM;48 小时) 抑制卵巢癌细胞系和原代培养物的生长。 RA-9 (1.25-5 μM;18 小时) 导致卵巢癌细胞中的细胞周期停滞和半胱天冬酶介导的细胞凋亡。 RA-9 (5 μM;0-24 小时) 诱导卵巢癌细胞中的内质网应激反应。 RA-9 (5 μM;超过 24 小时) 处理结果与时间依赖性的 PARP 切割形成的积累早在 8 小时就很明显。