RA375

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RA375 是 RPN13 (26S 蛋白酶体亚基) 抑制剂。RA375 激活 UPR 信号、ROS 产生和凋亡。RA375 的抗肿瘤活性是 RA190的 10 倍。

RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.

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RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice.Animal Model:RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice.Dosage:10 mg/kg.Administration:IP for a 5 days on, 2 days off cycle for two weeks.Result:Reduced ovarian tumor burden in mice.Animal Model:Female Balb/c mice.Dosage:5, 10, 20, 40, 60, 100 mg/kg (Pharmacological Analysis).Administration:IP single dose.Result:The dose of 40 mg/kg on alternate days for two weeks produced no observable toxicities or weight loss.

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Proteasome/Ubiquitin

Proteasome

Proteasome

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2649154-57-2

588.99

C30H25ClN4O7

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (169.78 mM; 超声助溶 )

O=C(CCl)N[C@H](C(N1C/C(C(/C(C1)=C/C2=CC=C([N+]([O-])=O)C=C2)=O)=C\C3=CC=C([N+]([O-])=O)C=C3)=O)CC4=CC=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years