l General Information |
Product Name | Omipalisib (GSK2126458, GSK458) |
General description | Omipalisib is a highly selective and potent inhibitor of p110α/β/δ/γ and mTORC1/2. |
Synonym | 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide |
Purity | ≥98.0%(HPLC) | CAS Number | 1086062-66-9 |
Formula | C25H17F2N5O3S | Molecular Weight | 505.5 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | solid |
Solubility(25℃) | DMSO | ≥50mg/mL |
Ethanol | Insoluble |
Water | Insoluble |
l Biological Information |
Biochem/Physiol
Actions | 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. |
Application | Omipalisib has been used in trials studying the treatment of CANCER, Solid Tumours, and Idiopathic Pulmonary Fibrosis. |
l Storage |
Storage temp. | -20℃ |
l Precautions and Disclaimer |
This
product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
