Catalog No.: PC-73424Not For Human Use, Lab Use Only.
Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.
Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.
Izorlisib (CH5132799) shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 >10 μM) against 26 protein kinases.
Izorlisib (CH5132799) exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα.
Izorlisib (CH5132799) effectively suppresses phosphorylation of Akt PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1 in breast cnacer KPL-4 cells.
Izorlisib (CH5132799) shows potent in vivo antitumor activity in several different xenograft models with PIK3CA mutations.
