|5-[2-[cis-2,6-二甲基-4-吗啉基]-4-(4-吗啉基)吡啶并[2,3-d]嘧啶-7-基]-2-甲氧基苯甲醇|CsnPharm

CAS No.: 938440-64-3

KU-0063794 Catalog No. CSN12392

Synonyms: Ku-0063794;KU-63794

KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively) with no effect on PI3Ks.

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:~10nM mTORC2

IC50:~10nM
描述The mTOR (mammalian target of rapamycin) protein kinase plays a key role in signalling pathways regulating cell growth and proliferation. There are two mTOR complexes characterized, mTORC1 and mTORC2. KU-0063794 is a specific mTORC1 and mTORC2 inhibitor (IC50=∼10 nM, assayed by activity of endogenous immunoprecipitated mTORC on its subtrates). Ku-0063794 can inhibit the downstream of mTORC1, pS6K-T229/389, pS6P-S235, as well as the downstream of mTORC2 pAKT-s473 and its substrates PRAS40 at Thr246, GSK3α/β at Ser21/Ser9 and Foxo-1/3a at Thr24/Thr32, at the concentration 30-1000nM in HEK-293 cell line culture in full media or under IGF1 stimulation. This demonstrates Ku-0063794 can inhibit both mTORC1 and 2 activity in vitro. Ku-0063794 can suppress growth of both wild-type and mLST8-deficient MEFs more markedly than rapamycin and increased the proportion of cells in G1 by 1.5-fold. ^[1]
作用机制KU-0063794 is an ATP competitive mTOR inhibitor. ^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
786-O	100-2000 nM	Function Assay	10-180 min	inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors	23349989
786-O	300-4000 nM	Cell Viability Assay	24-96 h	suppresses the cell viability in both time and dose dependent manner	23349989
786-O	2 µM	Function Assay	72 h	induces G1 cell cycle arrest and autophagy	23349989

更多
动物研究
剂量
Nude Mice: 8 mg/kg^[2]

给药途径
i.p.

动物研究
剂量	Nude Mice: 8 mg/kg^[2]
给药途径	i.p.

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
- 2.1480 mL
- 10.7401 mL
- 21.4802 mL
- 5 mM
- 0.4296 mL
- 2.1480 mL
- 4.2960 mL
- 10 mM
- 0.2148 mL
- 1.0740 mL
- 2.1480 mL

技术信息

CAS号

938440-64-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H31N5O4

运输

蓝冰

分子量

465.54

别名

Ku-0063794;KU-63794

溶解度

DMSO	33.0 mg/mL (70.9 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	0.66 mg/mL	clear
PO	0.5% CMC-Na	48 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

786-O	100-2000 nM	Function Assay	10-180 min	inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors	23349989
786-O	300-4000 nM	Cell Viability Assay	24-96 h	suppresses the cell viability in both time and dose dependent manner	23349989
786-O	2 µM	Function Assay	72 h	induces G1 cell cycle arrest and autophagy	23349989
AGS	-	Growth Inhibition Assay	-	IC50=15.0 ± 2.91 μM	24597478
Caki-1	100-2000 nM	Function Assay	10-180 min	inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors	23349989
Caki-1	300-4000 nM	Cell Viability Assay	24-96 h	suppresses the cell viability in both time and dose dependent manner	23349989
Caki-1	2 µM	Function Assay	72 h	induces G1 cell cycle arrest and autophagy	23349989
H1650	-	Growth Inhibition Assay	72 h	IC50=7.61±0.62 nM	23874880
H1650	7.61 nM	Function Assay	72 h	inhibits mTOR phosphorylation status	23874880
H1650	7.61 nM	Function Assay	72 h	inhibits phosphorylation of p70S6K	23874880
H1975	-	Growth Inhibition Assay	72 h	IC50=11.15±0.93 nM	23874880
H1975	11.15 nM	Function Assay	72 h	inhibits mTOR phosphorylation status	23874880
H1975	11.15 nM	Function Assay	72 h	inhibits phosphorylation of p70S6K	23874880
HepG2	0.1–50 μM	Cell Viability Assay	72 h	decreases cell viability in a dose dependent manner	26278819
HepG2	1–50 μM	Colony Formation Assay	10 d	decreases the number of viable HepG2 colonies significantly	26278819
HepG2	0.1–50 μM	Apoptosis Assay	48 h	induces apoptosis in a dose dependent manner	26278819
HepG2	5/10 μM	Function Assay	24 h	dramatically inhibits phosphorylation of AKT at Ser-473	26278819
HepG2	5/10 μM	Function Assay	24 h	downregulates the levels HIF1α and cyclin D1	26278819
HepG2	0.1–50 μM	Function Assay	24 h	induces p62 downregulation, Beclin-1 expression and LC3B-I to LC3B-II conversion in a dose dependent manner	26278819
HepG3	0.1–50 μM	Function Assay	48 h	induces cell autophagy in a dose dependent manner	26278819
HGC27	-	Growth Inhibition Assay	-	IC50=15.0 ± 4.82 μM	24597478
LNCaP	0-10 μM	Cell Viability Assay	24 h	decreases cell viability in a dose dependent manner	23840605
LNCaP	200–800 nM	Function Assay	24 h	decreases the phosphorylation level of p70S6K in a dose dependent manner	23840605
MDA-MB-468	0-10 μM	Cell Viability Assay	24 h	decreases cell viability in a dose dependent manner	23840605
MDA-MB-468	200–800 nM	Function Assay	24 h	decreases the phosphorylation level of p70S6K in a dose dependent manner	23840605
MKN45	-	Growth Inhibition Assay	-	IC50=0.82 ± 0.01 μM	24597478
NUGC4	-	Growth Inhibition Assay	-	IC50=2.93 ± 0.31 μM	24597478
PC-3	0-10 μM	Cell Viability Assay	24 h	decreases cell viability in a dose dependent manner	23840605
PC-3	200–800 nM	Function Assay	24 h	decreases the phosphorylation level of p70S6K in a dose dependent manner	23840605
PC9	-	Growth Inhibition Assay	72 h	IC50=10.15±0.62 nM	23874880
PC9	10.15 nM	Function Assay	72 h	inhibits mTOR phosphorylation status	23874880
PC9	10.15 nM	Function Assay	72 h	inhibits phosphorylation of p70S6K	23874880
PC9GR	-	Growth Inhibition Assay	72 h	IC50=6.21±1.30 nM	23874880
PC9GR	6.21 nM	Function Assay	72 h	inhibits mTOR phosphorylation status	23874880
PC9GR	6.21 nM	Function Assay	72 h	inhibits phosphorylation of p70S6K	23874880

靶点	Description	IC50
mTORC1		IC50:~10nM
mTORC2		IC50:~10nM

KU-0063794 Catalog No. CSN12392

靶点选择性

请登录您的专属账户

确认信息