PF-05212384 (PKI-587)
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.
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
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化学结构
