|反式-4-[4-氨基-5-(7-甲氧基-1H-吲哚-2-基)咪唑并[5,1-f][1,2,4]三嗪-7-基]环己烷羧酸|CsnPharm

CAS No.: 936890-98-1

OSI-027 Catalog No. CSN16065

Synonyms: ASP7486;ASP4786

OSI-027 shows the selective and ATP competitive inhibition activities against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

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

靶点 mTORC1

IC50:22nM mTORC2

IC50:65nM
描述The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that integrates with multiple pathways involving cell growth, survival and cancer physiology. OSI-027 is an ATP-competitive inhibitor of mTOR kinase with an IC₅₀ value of 4 nM. OSI-027 targeted both mTORC1 and mTORC2 , the two complexes of mTOR, with IC₅₀ values of 22 and 65 nM, respectively. In mechanistic cell assay, OSI-027 inhibited mTOR signaling of phospho-4E-BP1 with an IC₅₀ value of 1 μM. Treatment with OSI-027 (0.001 - 10 μΜ) dose-dependently suppressed Akt phosphorylation and the downstream substrate of Akt, PRAS40, in ovcar-3 ovarian carcinoma cells^[3]. In acute myeloid leukemia (AML) cells, OSI-027 blocked mTORC1 and mTORC2 activities at the concentration of 10 μΜ. The incubation with 10 μΜ OSI-027 also suppressed the mRNA translation of cyclin D1 and other proliferation-related genes in AML cells^[4]. In GEO colorectal xenograft mice, administration of OSI-027 (65 mg/kg) for 12 days inhibited both mTORC1 and mTORC2 effectors, and slowed the tumor growth as compared to the control group^[3].
作用机制OSI-027 is a ATP-competitive inhibitor of mTOR kinase.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human Caki1 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human Caki1 cells after 72 hrs by MTT assay, IC50=1.9 μM	24445311
human COLO205 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay, IC50=5.8 μM	24445311
human COLO205 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay	24836070

更多
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00698243	Any Solid Tumor or Lymphoma	Phase 1	Completed	-	United States, Michigan ... more >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Belgium University Hospitals Leuven Leuven, Belgium, 3000 United Kingdom Royal Mardsen Hospital Sutton, Surrey, United Kingdom, SM2 5PT Collapse <<

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
- 2.4604 mL
- 12.3020 mL
- 24.6040 mL
- 5 mM
- 0.4921 mL
- 2.4604 mL
- 4.9208 mL
- 10 mM
- 0.2460 mL
- 1.2302 mL
- 2.4604 mL

技术信息

CAS号

936890-98-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H22N6O3

运输

蓝冰

分子量

406.44

别名

ASP7486;ASP4786

溶解度

DMSO	175.0 mg/mL (430.6 mM)
Water	insoluble

动物实验配方

1% DMSO+30% polyethylene glycol+1% Tween 80+water

30 mg/mL

suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

OSI-027 Catalog No. CSN16065

靶点选择性

请登录您的专属账户

确认信息