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ICONC14284 Torin 1 (1222998-36-8 )
 
 
Catalog No.: C14284
CAS No.: 1222998-36-8
Synonym: Torin1; Torin-1
Chemical Name:
1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-benzo[h]-1,6-naphthyridin-2(1H)-one
Molecular Formula: C35H28F3N5O2
Molecular Weight: 607.62
 
Technical Data:
Appearance:
Solubility: Soluble in DMSO
Purity:
Storage: Store at +4°C
Original QC Data:
Shipping Conditions: Ambient Temp.
 
Price and Availability of Torin 1:

Size

Price

Stock

10mg 

USD

In Stock 

25mg 

USD

In Stock 

50mg 

USD

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Contact us for competitive discounts on bulk quantities

 
Biological Activity:

Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

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.

 
References:

1. Guertin and Sabatini (2009) The pharmacology of mTOR inhibition. Sci.Signal. 2 pe24.

2. Thoreen et al (2009) An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J.Biol.Chem. 284 8023.

 
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