GNE-317
mRNA synthesis
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.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GNE-317是PI3K的强效抑制剂[1]。
磷脂酰肌醇-4,5-二磷酸3-激酶(PI3K)是一系列酶,在细胞生长、增殖、分化、存活、运动和细胞内运输中起重要作用。
在GL261细胞系中,GNE-317具有细胞毒性[2]。
在小鼠脑中,50 mg/kg 的GNE-317显著抑制80%、84%和92%的pAkt、p4EBP1和pS6,这是PI3K/mTOR途径的下游标记物。在U87、GS2和GBM10荷瘤小鼠中,GNE-317分别抑制90%、50%和具有存活效果的肿瘤生长[1]。在接种GL261-GFP-Luc细胞的C57B6/J小鼠中,GNE-317在正常脑、肿瘤中心和肿瘤边缘的浓度没有明显不同。在荷瘤小鼠中,GNE-317显著降低肿瘤内p-AktSer473、p-S6Ser235/236 和p-4EBP1Thr37/46的水平[2]。在U87和GS2胶质母细胞瘤(GBM)模型中,GNE-317均匀地分布在脑中。GNE-317的脑-血浆比大于1,这与GNE-317的脑渗透特性一致[3]。
参考文献:
[1]. 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.
[2]. 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.
[3]. 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 |
M.Wt | 414.48 |
Cas No. | 1394076-92-6 |
Formula | C19H22N6O3S |
Solubility | Soluble in DMSO |
Chemical Name | 5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine |
SDF | Download SDF |
Canonical SMILES | COC1(COC1)C2=C(C)C3=C(S2)C(N4CCOCC4)=NC(C5=CN=C(N)N=C5)=N3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |