PF-4989216
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-4989216对p110α\p110β\p110γ\p110δ和VPS34的IC50值分别为2 nM\142 nM\65 nM\1 nM和110 nM.
在多种人类肿瘤中,PI3K p110a催化亚基基因突变或肿瘤抑制因子PTEN功能丧失诱导磷酸肌醇3-激酶(PI3K)组成性激活.小细胞肺癌患者具有极差的预后以及存活率,因而迫切需要接受有效的靶向治疗.PF-4989216是一种口服的PI3K选择性抑制剂.
体外:在携带PIK3CA突变的小细胞肺癌(SCLC)中,PF-4989216抑制PI3K下游信号传导\诱导细胞凋亡并且抑制细胞活力\转化以及异种移植肿瘤生长.在丢失PTEN的SCLC中,OF-4989216也抑制PI3K信号传导,但不会诱导BCL2相互作用介质介导的细胞凋亡,对细胞活力或转化也无任何作用[1].
体内:体内结果表明,PF-4989216在小鼠体内外的作用具有良好的相关性.此外,在携带PIK3CA突变的人SCLC肿瘤的小鼠中,PF-4989216显示出有效的抗肿瘤活性[1].
临床试验:到目前为止,OF-4989216还处于临床前开发阶段.
参考文献：
[1] Walls M, Baxi SM, Mehta PP, Liu KK, Zhu J, Estrella H, Li C, Zientek M, Zong Q, Smeal T, Yin MJ. Targeting small cell lung cancer harboring PIK3CA mutation with a selective oral PI3K inhibitor PF-4989216. Clin Cancer Res. 2014 Feb 1;20(3):631-43.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 380.4 |
| Cas No. | 1276553-09-3 |
| Formula | C18H13FN6OS |
| Solubility | Soluble in DMSO |
| Chemical Name | 4-(4-cyano-2-fluorophenyl)-2-morpholino-5-(1H-1,2,4-triazol-3-yl)thiophene-3-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | FC1=C(C(C(C#N)=C2N3CCOCC3)=C(S2)C4=NNC=N4)C=CC(C#N)=C1 |
| 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。 |
化学结构
