CH5132799
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.
CH5132799是一种I类磷脂酰肌醇-3-激酶(PI3K)抑制剂,对PI3Kα的IC50值为14 nM[1].
CH5132799对I类PI3K具有抑制效果,对PI3Kα\PI3Kβ\PI3Kδ和PI3Kγ的IC50值分别为0.014 μM\0.12 μM\0.5 μM和0.036 μM.PI3Kα对CH5132799尤为敏感.CH5132799是一种选择性抑制剂,对II类PI3K\III类PI3K和mTOR效果较差.对其他26种蛋白激酶,CH5132799的IC50值大于10 μM,几乎没有抑制能力.CH5132799具有有效的抗肿瘤活性,在HCT116\KPL-4\T-47D和SK-OV-3细胞系中的IC50值分别为0.2 μM\0.032 μM\0.056 μM和0.12 μM.此外,CH5132799在动物模型中口服可利用.在人类乳腺癌异种移植小鼠中,CH5132799在12.5 mg/kg剂量下体现出较强的肿瘤消退功能[1].
参考文献：
[1] Ohwada J, Ebiike H, Kawada H, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772.
| Storage | Store at -20°C |
| M.Wt | 377.42 |
| Cas No. | 1007207-67-1 |
| Formula | C15H19N7O3S |
| Solubility | Soluble in DMSO |
| Chemical Name | 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine |
| SDF | Download SDF |
| Canonical SMILES | CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N |
| 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 | CH5132799是一种I类PI3K抑制剂. | |||||
| 靶点 | PI3Kα | PI3Kγ | PI3Kβ | PI3Kδ | mTOR | |
| IC50 | 14 nM | 36 nM | 0.12 μM | 0.50 μM | 1.6 μM | |
化学结构
