Product Size
5 mg
25 mg
Custom Size
Product Overview
Description
Potent, selective mTOR inhibitor.
Biological Description
Potent, selective, ATP-competitive mTOR inhibitor. Inhibits mTORC1 (IC50 = 2.1 nM) in in vitro kinase activity assays. Displays 800-fold selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively). Attenuates phosphorylation of mTOR downstream targets, inhibits cell proliferation of several cancer cell types, and induces apoptosis and autophagy. Also exhibits potent biochemical and cellular activity against phosphatidylinositol-3 kinase-like kinase (PIKK) family kinases including ATM, ATR and DNA-PK (EC50 values are 28 nM, 35 nM and 118 nM respectively). Has significantly improved bioavailability (54%), metabolic stability, and plasma exposure compared to Torin 1.
Solubility Overview
Soluble in DMSO to 20 mM.
Chemical Properties
Chemical Name
9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]-benzo[h]-1,6-naphthyridin-2(1H)-one
Molecular Weight (Da)
432.40
Molecular Formula
C24H15F3N4O
SMILES
C1=CC(=CC(=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CN=C(C=C5)N)C(F)(F)F
Storage & Handling
Storage Instructions
Shipped at 4 °C. Store at -20 °C. Store under desiccating conditions.
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20 °C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
