PI-103

Short Summary : Class I PI3K, mTOR and DNA-PK inhibitor

Category : PI3K/Akt/mTOR Signaling|PI3K

Purity : 0.9866

CAS Number : 371935-74-9

Formula : C19H16N4O3

Molecular Weight : 348.36

SMILE : C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

Solubility : >17.4mg/mL in DMSO

Storage : Store at -20°C

Description : PI-103 is a potent and selective inhibitor of class I PI3K, mTOR and DNA-PK with IC50 values of 2, 3, 3, 15, 30 and 23 nM for p110, p110, p110, p110, mTOR and DNA-PK, respectively [1].PI-103 showed potent antiproliferation activities in various cancer cell lines such as prostate, ovary and glioblastoma. It exerted GI50 values of 0.14, 0.06, 0.13, 0.10, 0.12 and 0.08 M in U87MG, IGROV-1, DETROIT-562, PC3, SKOV-3 and HUVEC cells, respectively. In U87MG cells, 2 hour-treatment of PI-103 caused inhibition effects on various phosphorylated protein biomarkers of PI3K pathway with IC50 values of 15, 36, 111, 106 and 105 nM for p-AKTSer473, p-AKTThr308, p-GSK3Ser9, p-p70S6KThr421/Ser424 and p-S6RPSer235/Ser236, respectively [1]. References:[1] Raynaud F I, Eccles S A, Patel S, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Molecular cancer therapeutics, 2009, 8(7): 1725-1738.

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