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Omipalisib

商品编号: TS0014
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详细介绍

l  基本信息

产品名称

Omipalisib (GSK2126458, GSK458)

一般描述

Omipalisib is a highly selective and potent inhibitor of p110α/β/δ/γ and mTORC1/2.

别 称

2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide

纯 度

≥98.0%(HPLC)

CAS NO.

1086062-66-9

分子式

C25H17F2N5O3S

分子量

505.5

适用范围

生物试剂,适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25)

DMSO

≥50mg/mL

乙醇

Insoluble

Insoluble

l  生物学信息

生物活性/药理作用

Omipalisib is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity. Omipalisib binds to and inhibits PI3K in the PI3K/mTOR signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability and inducing apoptotic cell death. Bax is a member of the proapoptotic Bcl2 family of proteins. PI3K, often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.

Omipalisib is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively.

l  存储

存储温度

-20

l  注意事项及免责声明

本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov