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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 |
水 | 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 |