WYE-125132 (WYE-132)
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.
WYE-125132(WYE-132)是一种高效的ATP竞争性mTOR特异性抑制剂,IC50值为0.19±0.07 nmol/L,选择性是PI3Ks的5000多倍[1].
在免疫复合物试验中,WYE-125132(WYE-132)可抑制mTORC1依赖性的S6K(T389)磷酸化和mTORC2依赖性的AKT(S473)磷酸化.此外,在胰岛素样生长因子I(IGF-I)诱导的Rat1\PIK3CA突变的MDA361或PTEN缺失的U87MG细胞中,WYE-125132 (WYE-132)可剂量依赖地抑制P-S6K(T389)和P-AKT(S473),EC50为低纳摩尔级别.除此之外,WYE-125132 (WYE-132)是MDA361\PC3MM2\U87MG\A549和HCT116细胞系的有效抗增殖制剂.另外,WYE-125132 (WYE-132)在MDA361和HEK293细胞系中拥有更强的抑制蛋白合成和细胞大小的能力[1].
参考文献：
[1] Yu K1, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 519.61 |
| Cas No. | 1144068-46-1 |
| Formula | C27H33N7O4 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥13 mg/mL in DMSO |
| Chemical Name | 1-[4-[1-(1,4-dioxaspiro[4.5]decan-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-3-methylurea |
| SDF | Download SDF |
| Canonical SMILES | CNC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCC5(CC4)OCCO5)C(=N2)N6CC7CCC(C6)O7 |
| 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。 |
| Description | WYE-125132(WYE-132)是一种高效的ATP竞争性mTOR抑制剂,IC50值为0.19 nM. | |||||
| 靶点 | mTOR | |||||
| IC50 | 0.19 nM | |||||
化学结构
