GNE-477
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-477对PI3K和mTOR的IC50值分别为4 nmol/L和21 nmol/L。
GNE-477是一种有效的PI3K/mTOR双重抑制剂。PI3K/AKT/mTOR信号通路常与致癌恶性肿瘤相关,因而可作为有吸引力的靶点,用于研发其口服小分子抑制剂。
体外:GNE-477抑制PI3Kα、PI3Kβ、PI3Kδ以及PI3Kγ,其IC50值分别为4 nM、86 nM、6 nM和15 nM[1]。
体内:GNE-477及其去甲基类似物之间的直接比较表明,在大鼠体内,GNE-477清除率减少,此趋势同样存在于犬和小鼠中。在犬中,去甲基类似物清除显著增加,在肝血流中,其清除速率达2/3,而GNE-477清除率较低。在一项持续了10-14天的PC3肿瘤异种移植肿瘤生长抑制评估实验中,20 mg/kg GNE-477,每日1次,能使肿瘤停止生长,而1 mg/kg GNE-477,每日1次,可显著抑制肿瘤生长。相对于赋型剂组,GNE-477引起的体重减轻处于可接受水平,因而GNE-477耐受性良好[1]。
临床试验:N/A。
参考文献:
[1] Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J,Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11.
Storage | Desiccate at -20°C |
M.Wt | 504.63 |
Cas No. | 1032754-81-6 |
Formula | C21H28N8O3S2 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥16.69 mg/mL in DMSO with gentle warming |
Chemical Name | 5-(7-methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine |
SDF | Download SDF |
Canonical SMILES | O=S(N1CCN(CC2=C(C)C3=NC(C4=CN=C(N)N=C4)=NC(N5CCOCC5)=C3S2)CC1)(C)=O |
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。 |
质量控制和MSDS
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