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Product Details
Synonyms GNE490
Product Type Chemical
Formula C18H22N6O2S
MW 386.5
CAS 1033739-92-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: PI3K | Kinase Group: Lipid Kinase | Substrate: Lipid

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
GNE-490 is a highly selective pan-PI3K inhibitor that demonstrates selectivity over mTOR. It has good pharmacokinetic (PK) parameters and demonstrates knock down of pathway markers in vivo. Originally obtained via modification of compounds like GDC-0941, GNE-490 which have a significantly reduced potency mTOR while maintaining effective potency for PI3K substrates. IC(50) values for PI3K family members are in the subnanomolar to low nanomolar range (-.28 to < 20nm) while IC(50) values for mTOR and other related tyrosine kinases are greater than 750nM with most being greater than 1µM or more, thus GNE-490 makes a good choice for examining PI3K related events separate from those mediated by mTOR.
Product References
  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: D.P. Sutherlin, et al.; J. Med. Chem. 53, 1086 (2010)
  2. Design, synthesis and 3D-QSAR analysis of novel 2-hydrazinyl-4-morpholinothieno[3,2-d]pyrimidine derivatives as potential antitumor agents: W. Zhu, et al.; Eur. J. Med. Chem. 57, 162 (2012)
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