KU-0063794 | Specific mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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KU-0063794 99%+

货号：A119369

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.

KU-0063794 化学结构
CAS号：938440-64-3

KU-0063794 3D分子结构
CAS号：938440-64-3

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KU-0063794 纯度/质量文件产品仅供科研

货号：A119369 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

mTOR 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 nM				99%+
Gedatolisib	++++ mTOR, IC50: 1.6 nM				98%
GSK1059615	++ mTOR, IC50: 12 nM				98%
Vistusertib	+++ mTOR, IC50: 2.8 nM				99%+
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	99%+
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				98+%
PI-103	+ mTOR, IC50: 30 nM				99%+
WAY-600	++ mTOR, IC50: 9 nM				99%
Voxtalisib	+ mTOR, IC50: 157 nM				99%+
PF-04691502	++ mTOR, Ki: 16 nM				98+%
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	99%+
Chrysophanol	✔			EGFR	98%
Samotolisib	✔			DNA-PK	99%+
Torkinib	+++ mTOR, IC50: 8 nM			DNA-PK,PDGFR	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				98%
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			VEGFR,PDGFR	99%+
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	99%+
Rapamycin	++++ mTOR, IC50: ~0.1 nM				98%
GDC-0349	+++ mTOR, Ki: 3.8 nM				98%
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		99%+
WYE-687	+++ mTOR, IC50: 7 nM				98+%
Apitolisib	+ mTOR, Ki app: 17 nM				98%+
WYE-132	++++ mTOR, IC50: 0.19 nM				99%+
Sapanisertib	++++ mTOR, Ki: 1.4 nM				99%+
BGT226 maleate	✔				99%+
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	98%
PI3K-IN-1	+ mTOR, IC50: 157 nM				98+%
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				99+%
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		99%+
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				99%+
Temsirolimus	+ mTOR, IC50: 1.76 μM				99%
CZ415	++ mTOR, pIC50: 8.07				99%+
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	99%+
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		99%+
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		99%+
Palomid 529		✔			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

KU-0063794 生物活性

靶点	mTORC1 mTORC1, IC50:~10 nM mTORC2 mTORC2, IC50:~10 nM
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]

KU-0063794 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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

KU-0063794 动物研究

Dose	Nude Mice: 8 mg/kg^[2]
Administration	i.p.

KU-0063794 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL

KU-0063794 技术信息

CAS号	938440-64-3
分子式	C₂₅H₃₁N₅O₄
分子量	465.54

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 16 mg/mL(34.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

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

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

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

KU-0063794 99%+

KU-0063794 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

KU-0063794 质控信息

KU-0063794 生物活性

KU-0063794 细胞研究

KU-0063794 动物研究

KU-0063794 实验方案

KU-0063794 技术信息

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KU-0063794 99%+

KU-0063794 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

KU-0063794 质控信息

KU-0063794 生物活性

KU-0063794 细胞研究

KU-0063794 动物研究

KU-0063794 实验方案

KU-0063794 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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KU-0063794 纯度/质量文件产品仅供科研