GNE-490
| Code | Size | Price |
|---|
| SYN-1114-M100 | 100 mg | Enquire |
Quantity:
| SYN-1114-M050 | 50 mg | Enquire |
Quantity:
| SYN-1114-M001 | 1 mg | £233.00 |
Quantity:
| SYN-1114-M005 | 5 mg | £461.00 |
Quantity:
| SYN-1114-M010 | 10 mg | £643.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
GNE490
Appearance:
Solid.
CAS:
1033739-92-2
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C18H22N6O2S/c1-10-11(9-20-17(19)21-10)15-22-12-8-13(18(2,3)25)27-14(12)16(23-15)24-4-6-26-7-5-24/h8-9,25H,4-7H2,1-3H3,(H2,19,20,21)
InChiKey:
SFWTVVNNVHWDEE-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1033739-92-2. Formula: C18H22N6O2S. MW: 386.5. 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.
Molecular Formula:
C18H22N6O2S
Molecular Weight:
386.5
Package Type:
Plastic Vial
Product 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.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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