[CAS NO. 1222998-36-8]  Torin 1

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PRODUCTS SPECIFICATIONS [1222998-36-8]

Store
Catalog
SLK-S2827
Brand
Selleck
CAS
1222998-36-8

DESCRIPTION [1222998-36-8]

Overview

MDLMFCD18782653
Molecular Weight607.62
Molecular FormulaC35H28F3N5O2
SMILESO=C1N(C2=CC=C(N3CCN(C(CC)=O)CC3)C(C(F)(F)F)=C2)C4=C(C=NC5=CC=C(C6=CC7=CC=CC=C7N=C6)C=C54)C=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.6458 mL8.2288 mL16.4577 mL
5 mM0.3292 mL1.6458 mL3.2915 mL
10 mM---
50 mM---

Description

Torin 1 is a potent inhibitor of with of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

Targets


In vitro

Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. Moreover, Torin1 exhibits 1000-fold selectivity for mTOR over PI3K (EC50 = 1800 nM) and exhibits 100-fold binding selectivity relative to 450 other protein kinases. Torin1 causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2. Torin1 disrupts mTORC1-dependent phenotypes more completely than rapamycin. Rapamycin-resistant functions of mTORC1 are required for cap-dependent translation. In a recent study, it is reported Torin1 increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON.

In vivo

Torin1 is efficacious at a dose of 20 mg/kg in a U87MG xenograft model and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues.