RA-9,98.67%

产品编号:Bellancom-136528| CAS NO:919091-63-7| 分子式:C19H15N3O5| 分子量:365.34

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-136528
550.00 杭州 北京(现货)
Bellancom-136528
950.00 杭州 北京(现货)
Bellancom-136528
2400.00 杭州 北京(现货)
Bellancom-136528
4200.00 杭州 北京(现货)

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RA-9

产品介绍 RA-9 是一种高效选择性蛋白酶体相关 DUBs 抑制剂,具有良好的毒性和抗癌活性。RA-9 阻断泛素依赖性蛋白降解而不影响 20S 蛋白酶体蛋白水解活性。RA-9 选择性诱导卵巢癌细胞株和供体原代培养细胞凋亡。RA-9 诱导卵巢癌细胞内质网应激反应。
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.

体外研究

RA-9 (10-30 μM; 48 hours) inhibits growth of ovarian cancer cell lines and primary cultures.
RA-9 (1.25-5 μM; 18 hours) causes cell cycle arrest and caspase-mediated apoptosis in ovarian cancer cells.
RA-9 (5 μM; 0-24 hours) induces ER-stress responses in ovarian cancer cells.
RA-9 (5 μM; over 24 hours) treatment results with time-dependent accumulation of the cleaved formed of PARP noticeable as early as 8 hours.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: Cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2, Cisplatin-resistant ovarian cancer cell lines HEY and OVCAR-3, primary ovarian cancer cells
Concentration: 10, 20, 30 μM
Incubation Time: 48 hours
Result: Compromised the viability of ovarian cancer cells in a dose-dependent fashion.

Cell Cycle Analysis

Cell Line: ES-2 cells
Concentration: 1.25, 5 μM
Incubation Time: 18 hours
Result: Resulted in a dose-dependent increase in the fraction of ES-2 cells in the G2-M cell cycle phase.

Western Blot Analysis

Cell Line: ES-2, SKOV-3 and TOV-21G ovarian cancer cells
Concentration: 5 μM
Incubation Time: 0-24 h
Result: Caused a time-dependent increase in the steady levels of the early ER-stress marker GRP-78, as well as the late ER-stress markers IRE1-α and Ero1L-α.
体内研究
(In Vivo)

RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究

RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究

RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
溶解性数据
In Vitro: 

DMSO : 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7372 mL 13.6859 mL 27.3718 mL
5 mM 0.5474 mL 2.7372 mL 5.4744 mL
10 mM 0.2737 mL 1.3686 mL 2.7372 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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