PI-103 Hydrochloride

CEI-1479

PI-103 is a dual inhibitor of PI3K/Akt and mTOR with IC50 value of 0.002 μM, 0.003μM, 0.003μM, 0.015μM, 0.030μM for P110α, P110β, P110γ, P110 and mTOR, respectively. PI3K/AKT/mTOR pathway is an intracellular signaling pathway and plays an important role in regulating cell cycle. It has been shown that PI3K/AKT/MTOR pathway is directly related to cellular quiescence, proliferation, cancer, and longevity. And many studies have shown that activation of the PI3K/Akt signaling pathway is correlated with poor prognosis in a variety of cancers which demonstrated that inhibition of the pathway may be regarded as a promising therapy. PI-103 is a selective PI3K/Akt and mTORC1 inhibitor. When tested with leukemic cell lines (MOLM14, OCI-AML3 and MV4-11) with activation of PI3K/Akt, mTORC1and ERK/MAPK signaling pathways, PI-103 blocked cells proliferation via inhibiting PI3K/Akt and mTORC1 activity in a concentration of 1μM. In HCC cell line--Huh7 cells, treated PI-103 alone or combined with sorafenib inhibited cells proliferation in a dose-dependent manner through inhibition of PI3K/Akt and mTORC1 pathways. When tested with U87MG glioblastoma cells, PI-103 treatment in 30 nM/L showed significant inhibition of PI3K/Akt and mTORC1 phosphorylation. In neuroblastoma cell lines SK-N-BE (2), IMR-32 with amplified MYCN, PI-103 inhibited cell growth in a time-and concentration-dependent manner via inhibiting PI3K/Akt and mTORC1 activity. In SK-N-BE (2) with MYCN-mutant xenografted nude mice model, treated PI-103 intraperitoneally (10 mg/kg) markedly reduced the tumor volume index and tumor weight via inhibiting PI3K/ mTOR pathways.

371935-79-4

384.82

0.98

Store at -20°C

PI 103 hydrochloride; PI103 hydrochloride

DNA-PK/PI 3-kinase/mTOR

C19H17ClN4O3

3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol; hydrochloride

Soluble in DMSO > 10 mM

Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request