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GNE-493

Catalog No. T7166 CAS 1033735-94-2

GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively.

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

GNE-493, CAS 1033735-94-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
2 mg	In stock	$ 169.00
5 mg	In stock	$ 288.00
10 mg	In stock	$ 377.00
25 mg	In stock	$ 623.00
50 mg	In stock	$ 878.00
100 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 317.00

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Purity: 98%

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Description	GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively.
Targets&IC50	mTOR:32 nM, PI3Kγ:16 nM , PI3Kα:3.4 nM , PI3Kβ:12 nM , PI3Kδ:16 nM
In vivo	GNE-493 was tested in a human MCF7.1 breast cancer xenograft model with a PI3Kα activating mutation. Mice with xenografts received a daily oral dose of 10 mg/kg of GNE-493 for 21 continuous days. Comparable to results in the PC3 prostate cancer model, this treatment led to a 73% inhibition of tumor growth by day 21 compared to control. With similar drug exposure levels, GNE-493 demonstrated equivalent suppression of the PI3K pathway and, thus, comparable efficacy against MCF7.1 breast tumors.

Molecular Weight	372.44
Formula	C17H20N6O2S
CAS No.	1033735-94-2

Storage

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

Solubility Information

DMSO: 45 mg/mL (120.82 mM)

References and Literature

1. Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer[J]. Journal of Medicinal Chemistry, 2010, 53(3):1086-1097.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Prostate Cancer Compound Library Orally Active Compound Library Autophagy Compound Library Oxidation-Reduction Compound Library Metabolism Compound Library PI3K-AKT-mTOR Compound Library Antioxidant Compound Library

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Keywords

GNE-493 1033735-94-2 PI3K/Akt/mTOR signaling mTOR PI3K Mammalian target of Rapamycin GNE493 Inhibitor inhibit Phosphoinositide 3-kinase GNE 493 inhibitor

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