WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205480
Description: Omipalisib, also known as GSK2126458, is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor GSK2126458 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.
MedKoo Cat#: 205480
Chemical Formula: C25H17F2N5O3S
Exact Mass: 505.10202
Molecular Weight: 505.5
Elemental Analysis: C, 59.40; H, 3.39; F, 7.52; N, 13.85; O, 9.50; S, 6.34
Synonym: GSK2126458; GSK-2126458; GSK 2126458; Omipalisib
IUPAC/Chemical Name: 2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide
InChi Key: CGBJSGAELGCMKE-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
SMILES Code: O=S(C1=CC=C(F)C=C1F)(NC2=CC(C3=CC=C4N=CC=C(C5=CC=NN=C5)C4=C3)=CN=C2OC)=O
GSK2126458 is a highly potent PI3K and mTOR inhibitor. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase