PI-103 is a potent PI3K and mTOR inhibitor with IC50 s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy [1] [2] [3] [4]. PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines [1].

2008年6月12日 · PI-103 is a new potent PI3K/Akt and mTOR inhibitor. In human leukemic cell lines and in primary blast cells from AML patients, PI-103 inhibited constitutive and...

PI-103 is an organic heterotricyclic compound that is pyrido [3',2':4,5]furo [3,2-d]pyrimidine substituted at positions 2 and 4 by 3-hydroxyphenyl and morpholin-4-yl groups respectively. A dual-kinase inhibitor with anti-cancer properties.

PI-103 是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于 p110α/β/δ/γ 的 IC50 为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小， IC50 为30 nM/23 nM。 PI-103 可诱导小鼠T细胞淋巴瘤的凋亡。

结论 PI-103 能够调节细胞周期蛋白阻滞喉鳞癌细胞周期,促进细胞死亡,抑制细胞迁移及侵袭,且效果优于单靶点抑制剂LY294002和Rapamycin,对头颈部鳞癌的临床治疗有潜在的研究价值。

PI-103 is a new potent PI3K/Akt and mTOR inhibitor. In human leukemic cell lines and in primary blast cells from AML patients, PI-103 inhibited constitutive and growth factor-induced PI3K/Akt and mTORC1 activation. PI-103 was essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase.

PI-103 A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.; CAS Number: 371935-74-9; Synonyms: …

2007年11月16日 · PI-103 dramatically inhibited both basal and growth factor-stimulated proliferation of blast cells. Interestingly, PI-103 induced significant apoptosis in 6 AML samples at 1µM and a significant decrease of CFU-L colonies in 6 other AML samples.

2007年11月16日 · PI-103 dramatically inhibited both basal and growth factor-stimulated proliferation of blast cells. Interestingly, PI-103 induced significant apoptosis in 6 AML samples …