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GSK1059615

Catalog No.
B2176
PI3K and mTOR inhibitor,potent and reversible
Grouped product items
SizePriceStock Qty
5mg
$80.00
In stock
10mg
$115.00
In stock
25mg
$270.00
In stock
50mg
$495.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GSK1059615 is inhibitor of pan-PI3K with IC50 values of 0.4nM, 0.6nM, 5nM, 2nM and 12nM for PI3Kα, P13Kβ, P13Kγ, P13Kδ and mTOR, respectively [1].

GSK1059615 is a potent and reversible inhibitor of P13K. It also has inhibition efficacy to the oncogenic mutants of PI3Kα. The thiazolidinedione ring of GSK1059615 forms an interaction with the catalytic lysine (Lys833) within the ATP-binding pocket. In cellular assay, GSK1059615 is reported to induce G1 arrest and apoptosis in a variety of cell lines. Among these, the breast tumor cells display more sensitive. Moreover, GSK1059615 significantly suppresses tumor growth and increases plasma insulin levels in xenograft mice [1, 2].

References:
[1] Carnero A. Novel inhibitors of the PI3K family. 2009.
[2] Knight S D, Adams N D, Burgess J L, et al. Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Medicinal Chemistry Letters, 2010, 1(1): 39-43.

Chemical Properties

StorageStore at -20°C
M.Wt333.36
Cas No.958852-01-2
FormulaC18H11N3O2S
Solubility≥8.3mg/mL in DMSO with gentle warming
Chemical Name(5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione
SDFDownload SDF
Canonical SMILESC1=CC2=NC=CC(=C2C=C1C=C3C(=O)NC(=O)S3)C4=CC=NC=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 values of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
Targets PI3Kα PI3Kβ PI3Kδ PI3Kγ mTOR  
IC50 0.4 nM 0.6 nM 2 nM 5 nM 12 nM  

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