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CAS No.: 1223001-51-1

Torin 2 Catalog No. CSN15687

Synonyms: Torin 2

Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM, showing 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties and inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively.

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400-920-2911

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400-920-2911

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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 ATM

EC50:28nM ATR

EC50:35nM DNA-PK

EC50:118nM mTOR

IC50:0.25nM
描述The mammalian target of rapamycin (mTOR) is a a key element in the PI3K/AKT/mTOR signal pathway, which is a member of PIKKk inase family, including PI3K, ATR, ATM, DNA-PK and SMG-1. Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53-/- MEFs cell line that is 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM, 35 nM, 118 nM, respectively, can be observed in PC3 cell lines. TFEB–GFP HeLa cells were treated with 10 different concentrations of the ERK inhibitor U0126, or the mTOR inhibitors including Torin 2 with the concentrations ranging from 2.54 nM to 50 μM, TFEB nuclear/cytoplasmic distribution for each concentration of each compound in duplicate represented as dose–response curves using a non-linear regression fitting. MZ-CRC-1 and TT cells were treated with inhibitor complexity including 100nM Torin 2. At 24 hours, Torin 2 exerted a significant reduction of migration of both cell types. Besides, concomitant expression of ALK^F1174L abrogated any efficacy of Torin2, as indicated by essentially stable tumor volumes after 7 days of treatment with this agent at 20 mg/kg/day, which in large part led to down-regulation of the mTORC1 targets, pS6K and p4E-BP1, but did not affect pMEK or pERK, or induce any substantial increase in apoptosis. Treatment with crizotinib and Torin2 significantly prolonged survival compared to the outcome with use of vehicle or either single agent alone, whereas mice treated with crizotinib and Torin2 as single agents began to die before treatment was stopped, suggesting Torin 2 can be helpful to inhibit the downstream pathways utilized by ALK^F1174L and MYCN.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human PC3 cells	-	Function assay	-	Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting, EC50=0.2 μM	21322566

动物研究

剂量

Mice: 2 mg/kg - 10 mg/kg^[3] (i.p.), 40 mg/kg^[4] (p.o.), 1 mg/kg^[2] (i.v.)

给药途径

i.p., p.o., i.v.

动物药代数据

Animal	Mice^[2]
Dose	1 mg/kg (i.v.) 10 mg/kg (p.o.)
F	51% (p.o.)
T_1/2	0.72 h (i.v.)
T_max	0.25 h (p.o.)
C_max	1540 ng/ml (i.v.) 3968 ng/ml (p.o.)
CL	19.6 ml/min/kg (i.v.)
Vss	1.0 L/kg (i.v.)
AUC	850 h·ng/ml (i.v.) 4311 h·ng/ml (p.o.)

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
NCT01801345	Fatigue	Not Applicable	Completed	-	United States, Illinois ... more >> Evanston Hospital Evanston, Illinois, United States, 60201 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
- 2.3127 mL
- 11.5634 mL
- 23.1269 mL
- 5 mM
- 0.4625 mL
- 2.3127 mL
- 4.6254 mL
- 10 mM
- 0.2313 mL
- 1.1563 mL
- 2.3127 mL

技术信息

CAS号

1223001-51-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H15F3N4O

运输

蓝冰

分子量

432.40

别名

Torin 2

溶解度

DMSO	50.0 mg/mL (115.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	35 mg/mL	suspension

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靶点	Description	IC50
ATM		EC50:28nM
ATR		EC50:35nM
DNA-PK		EC50:118nM
mTOR		IC50:0.25nM

Torin 2 Catalog No. CSN15687

靶点选择性

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