|N-((2-羟基萘-1-基)亚甲基)噻吩-2-磺酰胺|CsnPharm

CAS No.: 307543-71-1

STF-083010 Catalog No. CSN18196

Synonyms: IRE1 Inhibitor I

STF-083010 is a potent IRE1α endonuclease inhibitor which can block endogenous XBP1 mRNA splicing.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述STF-083010 is a novel Ire1 inhibitor which can Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. STF-083010 at 60μM inhibited endogenous XBP1 mRNA splicing in RPMI 8226 cells treated with 300nM thapsigargin. It inhibited the production of sXBP1 protein, but not the autophosphorylation of Ire1α, at 60μM in MM1.S and RPMI 8226 cell lines treated with 300nM thapsigargin. STF-083010 at 60mg/kg blocked bortezomib (1mg/kg)-induced XBP1 activity in vivo. Administration of STF-083010 at 30mg/kg, i.p., once weekly for 2 weeks, decreased tumor growth of NOD/SCID/IL2R_γ null mice xenograft RPMI 8226 tumor. STF-083010 was preferentially toxic to freshly isolated human CD138⁺ MM cells compared with other similarly isolated cell populations^[2].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
SF21 cell	-	Function assay	-	Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM	24749861

动物研究
剂量
Rat: 15 mg/kg^[2] (i.p.), 60 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 15 mg/kg^[2] (i.p.), 60 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Papandreou I, Denko NC, et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4.
[2] Papandreou I, Denko NC, Olson M, Van Melckebeke H, Lust S, Tam A, Solow-Cordero DE, Bouley DM, Offner F, Niwa M, Koong AC. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4. doi: 10.1182/blood-2010-08-303099. Epub 2010 Nov 16. PMID: 21081713; PMCID: PMC3056474.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1508 mL
- 15.7539 mL
- 31.5077 mL
- 5 mM
- 0.6302 mL
- 3.1508 mL
- 6.3015 mL
- 10 mM
- 0.3151 mL
- 1.5754 mL
- 3.1508 mL

技术信息

CAS号

307543-71-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H11NO3S2

运输

蓝冰

分子量

317.38

别名

IRE1 Inhibitor I

溶解度

DMSO	62.0 mg/mL (195.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+40%PEG 300+5% Tween80 +water

2 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

STF-083010 Catalog No. CSN18196

靶点选择性

请登录您的专属账户

确认信息