In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GNE-317 is a potent inhibitor of PI3K .
Phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) are a series of enzymes and play an important role in cell growth, proliferation, differentiation, survival, motility and intracellular trafficking.
In the GL261 cell line, GNE-317 showed cytotoxic activity .
In mouse brain, GNE-317(50 mg/kg) significantly inhibited pAkt, p4EBP1 and pS6 by 80%, 84%, and 92% respectively, which were downstream markers of the PI3K/mTOR pathway. In U87, GS2 and GBM10 tumor-bearing mice, GNE-317 inhibited tumor growth by 90%, 50% and a survival benefit, respectively . In C57B6/J mice inoculated with GL261-GFP-Luc cells, the concentrations of GNE-317 in the normal brain, tumor core and rim were not significantly different. In tumor-bearing mice, GNE-317 significantly reduced the levels of p-AktSer473, p-S6Ser235/236 and p-4EBP1Thr37/46 within the tumor . In U87 and GS2 glioblastoma multiforme (GBM) models, GNE-317 was uniformly distributed in the brain. The brain-to-plasma ratios for GNE-317 were greater than 1, in agreement with the brain penetration properties of GNE-317 .
. Salphati L, Heffron TP, Alicke B, et al. Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier. Clin Cancer Res, 2012, 18(22): 6239-6248.
. Becker CM, Oberoi RK, McFarren SJ, et al. Decreased affinity for efflux transporters increases brain penetrance and molecular targeting of a PI3K/mTOR inhibitor in a mouse model of glioblastoma. Neuro Oncol, 2015, pii: nov081.
. Salphati L, Shahidi-Latham S, Quiason C, et al. Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging. Drug Metab Dispos, 2014, 42(7): 1110-1116.
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|