PF-05212384 (PKI-587)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF-05212384是PI3K/mTOR的抑制剂,对PI3Kα\PI3Kβ\PI3Kγ\PI3Kδ和mTOR的IC50值分别为0.4 nM\6 nM\8 nM\6 nM和1.4 nM[1].
PF-05212384是一种pan-PI3K/mTOR抑制剂,对PI3K和mTOR具有高选择性.除了野生型PI3K,PF-05212384也可抑制突变型P13K,对H1047R和E545K突变体的IC50值均为6 nM.在细胞试验中,PF-05212384可在MDA-361和PC3-MM2细胞系中有效抑制肿瘤生长,IC50值分别为4 nM和13.1 nM.同时,PF-05212384可在细胞中抑制PI3K/mTOR信号通路蛋白磷酸化.该物质可抑制Akt和Akt效应蛋白包括GSK3激酶\ENOS和PRAS 40的磷酸化.此外,PF-05212384在包括H1975\BT474\HCT116\H1975和U87MG在内的多个异种移植模型中具有有效的抗肿瘤活性[1,2].
参考文献:
[1] Venkatesan A M, Dehnhardt C M, Delos Santos E, et al. Bis (morpholino-1, 3, 5-triazine) derivatives: potent adenosine 5’-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. Journal of medicinal chemistry, 2010, 53(6): 2636-2645.
[2] Mallon R, Feldberg L R, Lucas J, et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clinical Cancer Research, 2011, 17(10): 3193-3203.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 615.73 |
Cas No. | 1197160-78-3 |
Formula | C32H41N9O4 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥15.4 mg/mL in DMSO with gentle warming |
Chemical Name | 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea |
SDF | Download SDF |
Canonical SMILES | CN(C)C1CCN(CC1)C(=O)C2=CC=C(C=C2)NC(=O)NC3=CC=C(C=C3)C4=NC(=NC(=N4)N5CCOCC5)N6CCOCC6 |
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 | PF-05212384(PKI-587)是一种高效的PI3Kα\PI3Kγ和mTOR双重抑制剂,IC50值分别为0.4 nM\5.4 nM和1.6 nM. | |||||
靶点 | PI3Kα | mTOR | PI3Kγ | |||
IC50 | 0.4 nM | 1.6 nM | 5.4 nM |
质量控制和MSDS
- 批次:
化学结构
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