PKI-402
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.
PKI-402是选择性的\等效的和ATP竞争性的I类PI3K抑制剂(对PI3Kα/β/γ/δ的IC50值分别为1 nM/7 nM/16 nM/14 nM).
PI3K(磷脂酰肌醇-4,5-二磷酸-3-激酶)是一类酶家族,参与细胞功能,如细胞生长\增殖\分化\运动\存活和胞内运输,从而也参与癌症.PI3K在PI3K/Akt/mTOR通路中起重要作用.
在多种人类癌细胞系(如乳腺癌\脑瘤\胰腺癌和非小细胞肺癌)中,PKI-402抑制癌细胞生长,降低PI3K和mTOR效应分子的磷酸化.在MDA-MB-361中,30 nM PKI-402引起凋亡标志物PARP的裂解.
在MDA-MB-361小鼠肿瘤异种移植模型中,按100 mg/kg每天一次给予PKI-402共5天,能够将初始肿瘤体积从260 mm3降至129 mm3,并且在70天内抑制肿瘤的再生长,单剂量PKI-402阻断Akt磷酸化,造成PARP裂解.
参考文献：
1. Mallon R, Hollander I, Feldberg L et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 570.65 |
| Cas No. | 1173204-81-3 |
| Formula | C29H34N10O3 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥14.28 mg/mL in DMSO |
| Chemical Name | 1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea |
| SDF | Download SDF |
| Canonical SMILES | CCN1C2=C(C(=NC(=N2)C3=CC=C(C=C3)NC(=O)NC4=CC=C(C=C4)C(=O)N5CCN(CC5)C)N6CCOCC6)N=N1 |
| 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 | PKI-402是高效的PI3K/mTOR双重抑制剂,对PI3Kα/β/γ/δ和mTOR的IC50值分别为2 nM/7 nM/16 nM/14 nM和3 nM. | |||||
| 靶点 | PI3Kα | mTOR | PI3Kβ | PI3Kδ | PI3Kγ | |
| IC50 | 2 nM | 3 nM | 7 nM | 14 nM | 16 nM | |
化学结构
