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GSK1059615

Chemical Structure : GSK1059615

CAS No.: 958852-01-2

GSK1059615 (GSK 1059615;GSK-1059615)

Catalog No.: PC-42850Not For Human Use, Lab Use Only.

GSK1059615 is a highly potent, dual PI3K/mTOR inhibitor with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM for PI3Kα/β/δ/γ and mTOR, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK1059615 is a highly potent, dual PI3K/mTOR inhibitor with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM for PI3Kα/β/δ/γ and mTOR, respectively.
GSK1059615 inhibits survival and proliferation of established (SCC-9, SQ20B and A253 lines) and primary human HNSCC cells.
GSK1059615 blocks PI3K-AKT-mTOR activation in HNSCC cells, induces programmed necrosis but not apoptosis, suppresses SCC-9 tumor growth in nude mice.
GSK1059615 strongly reduces neutrophil-sperm interaction with IC50 of <10 nM in cattle.

Physicochemical Properties

M.Wt 333.3638
Formula C18H11N3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,4-Thiazolidinedione, 5-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-, (5Z)-

References

1. Carnero A. et al. Expert Opin Investig Drugs. 2009 Sep;18(9):1265-77.

2. Xie J, et al. Oncotarget. 2017 Feb 7;8(31):50814-50823.

3. Leontieva OV, et al. Aging (Albany NY). 2016 Dec 30;8(12):3535-3551.

4. Hong J, et al. Biol Reprod. 2017 Nov 1;97(5):671-687.

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