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SynKinase
GNE-490
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | GNE490 |
| Product Type | Chemical |
| Properties | |
| 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. |
| InChi Key | SFWTVVNNVHWDEE-UHFFFAOYSA-N |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
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
- 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)
- 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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