Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Cas No.||1276105-89-5||SDF||Download SDF|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
CNX1351 is a potent and selective inhibitor of PI3Kα with IC50 value of 6.8 nM  .
Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylating the 3’-hydroxyl group of phosphatidylinositol-4,5-bisphosphate (PIP2) to produce phosphatidylinositol-3,4,5-trisphosphate (PIP3). PI3Ks plays important roles in cell proliferation, survival, differentiation and metabolism  .
CNX1351 is a specific and covalent PI3Kα inhibitor. CNX1351 time-dependently and irreversibly inhibited PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with IC50 values of 6.8, 166.0, 240.3 and 3020.0 nM, respectively. In SKOV3 ovarian cancer cells with a mutation in PIK3CA that resulted in a constitutively activated PI3Kα, CNX1351 inhibited PI3K signaling with EC50 values of 10-100 nM. In MCF-7 breast cancer cells (E545K) and SKOV3 ovarian cancer cells (H1047R) with different PIK3CA activating mutations, CNX1351 inhibited cell growth with GI50 values of 55 and 78 nM, respectively .
In nude mice, CNX1351 (100 mg/kg ip) irreversibly bonded to p110α and inhibited P-AktSer473 expression .
. Nacht M, Qiao L, Sheets MP, et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J Med Chem, 2013, 56(3): 712-721.
. Jeong Y, Kwon D, Hong S. Selective and potent small-molecule inhibitors of PI3Ks. Future Med Chem, 2014, 6(7): 737-756.