您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > STF-083010
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
STF-083010
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STF-083010图片
CAS NO:307543-71-1
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
STF083010
产品介绍
STF083010 是一种 IRE1α 核酸内切酶的选择性抑制剂。

产品描述

STF-083010 is a selective inhibitor of the IRE1α endonuclease.

体外活性

WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 hours cultures. In MM.1R MM, MM.1S, and RPMI 8226 cell lines, STF-083010 displays cytostatic and cytotoxic activity in a dose and time-dependent manner. In Eμ-TCL1 CLL cells, STF-083010 displays about 70% growth inhibition after 3 days culture. In SU8686, Panc0403, and MiaPaCa2 cell lines, STF-083010 blocks IRE1α's endonuclease and inhibits XBP1 splicing activity without affecting its kinase activity.

体内活性

STF-083010 (i.p., 30 mg/kg) signi?cantly inhibits the growth of the tumor in human multiple myeloma (MM) xenografts model.

激酶实验

Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography.

细胞实验

3×10E3 (Panc0403, Panc1005, BxPc3, and MiaPaCa2) cell lines are seeded in 96-well plates overnight, and STF-083010(~50 μM) treatment for 48 hours started the next day.

动物实验

NOD/SCID/IL2Rγ null mice were injected intraperitoneally of STF-083010(30 mg/kg) dissolved in 16% chremophor.

Cas No.

307543-71-1

分子式

C15H11NO3S2

分子量

317.38

别名

STF083010

储存和溶解度

DMSO:31.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years