Cat No:LP000051
Product Name: GSK2126458;Omipalisib
CAS NO:1086062-66-9
Molecular Formula:C25H17F2N5O3S
Molecular Weight: 505.49600
Purity: ≥98%
Solubility: In DMSO
Storage: -10°C
GSK2126458 potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki of 8 pM, 8 pM and 9 pM, respectively. GSK2126458 causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively[1]. The combination of GSK2118436 or GSK1120212 with GSK2126458 enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines[2]. GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines.
