IITZ-01

1807988-47-1

C26H23FN8O

H2O : < 0.1 mg/mL (insoluble); DMSO : 150 mg/mL (310.87 mM; Need ultrasonic)

PI3K/Akt/mTOR; Autophagy

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC₅₀ of 2.62 uM for PI3Kgamma. IC50 & Target: IC50: 2.62 uM (PI3Kgamma), Autophagy^[1]. In Vitro: IITZ-01 (0-2 uM, 24 h) enhances autophagosomes formation as indicated by increased expression of LC3-II levels time- and dose-dependently in triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). IITZ-01 also demonstrates potent autophagy inhibitory activity in other breast, lung, and colon cancer cells^[1]. In Vivo: IITZ-01 (45 mg/kg, i.p. every alternate day for 4 weeks) inhibits average breast tumor growth when compared with control from third day of treatment in triple-negative breast tumor models in mice^[1].