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GSK1059615

Catalog No. T2357 CAS 958852-01-2

Synonyms: GSK 1059615, GSK-1059615

GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK1059615, CAS 958852-01-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 203.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 98%

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Description	GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
Targets&IC50	mTOR:12 nM, PI3Kγ:5 nM, PI3Kα:0.4 nM, PI3Kβ:0.6 nM, PI3Kδ:2 nM
Kinase Assay	HTRF In vitro Profiling Assays for PI3K Inhibition: The measurement of the GSK1059615-dependent inhibition of the PI3Ks is accessed using a HTRF based PI3K profiling assay kit. 400 pM enzyme is used in PI3Kα and δ assays, 200 pM in PI3Kβ assays, and 1 nM in PI3Kγ assay. In addition, the PI3Kα, β, and δ assays are run with 150 mM NaCl and 100 μM ATP, while the PI3Kγ assay is run with no NaCl and 15 μM ATP. All reactions are run at 10 μM PIP2. GSK1059615 is serially diluted (3-fold in DMSO), and 50 nL is transferred to a 384-well low-volume assay plate. PI3K Reaction Buffer is prepared by diluting the stock 1:4 with de-ionized water. Freshly prepared DTT is added at a final concentration of 5 mM on the day of use. Enzyme addition and GSK1059615 pre-incubation are initiated by the addition of 2.5 μL of PI3K in reaction buffer. Plates are incubated at room temperature for 15 min. Reactions are initiated by addition of 2.5 μL of 2× substrate solution (PIP2 and ATP in 1× reaction buffer). Plates are incubated at room temperature for one hour. Reactions are quenched by the addition of 2.5 μL of stop solution. The quenched reactions are then processed to detect product formation by adding 2.5 μL of Detection Solution. Following a 1-hour incubation in the dark, the HTRF signal is measured on the Envision plate reader set for 330 nM excitation and dual emission detection at 620 nM (Eu) and 665 nM (APC). The IC50 value is then obtained.
Cell Research	Cells are plate at a density of 1 × 104 cells per well in clear flat-bottomed 96-well plates and incubated overnight. Then, GSK1059615 is added and the plates are incubated for 30 min. At the end of incubation, media is aspirated from the plates, and the plate is wash once with cold PBS. 80 μL MSD Lysis buffer is added into each well and the plates are incubated on a shaker at 4 °C for at least 30 min. For Akt duplex assay, plates are washed with 200 μL/well wash buffer for 4 times and tapped on paper towel to blot. Then, 60 μL lysates is added to each well and the plates are incubated on shaker at room temperature for 1 hour. After another 4 times washing, antibody is added (25 μL per well) and the plates are incubated on shaker for 1 hour and washed again. Finally, Read Buffer is added (150 μL per well) and the plates are read immediately. IC50 values are then obtained.(Only for Reference)

Synonyms	GSK 1059615, GSK-1059615
Molecular Weight	333.36
Formula	C18H11N3O2S
CAS No.	958852-01-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.3 mg/mL (10 mM)

References and Literature

1. Carnero A. Expert Opin Investig Drugs, 2009, 18(9), 1265-1277. 2. Auger KR, et al. EORTC-NCI-AACR, 2008. 3. Bei S, et al. Inhibition of gastric cancer cell growth by a PI3K-mTOR dual inhibitor GSK1059615. Biochem Biophys Res Commun. 2019 Mar 26;511(1):13-20. 4. Knight SD, et al. ACS Med Chem Lett, 2010, 1(1), 39-43.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Neural Regeneration Compound Library PI3K-AKT-mTOR Compound Library Anti-Diabetic Compound Library Pyroptosis Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK1059615 958852-01-2 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR inhibit Mammalian target of Rapamycin Phosphoinositide 3-kinase GSK 1059615 Inhibitor GSK-1059615 inhibitor

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