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Table 2 Small-molecule compounds inhibiting CSC progression through suppressing Notch signaling pathway

From: Emerging agents that target signaling pathways in cancer stem cells

Name Target Mechanism Type of cancer Phase NCT number (starting time)/publication date Assessment
MK-0752 γ-secretase Decreases the population of CD44+/CD24 and ALDH+, reduces mammosphere-forming efficiency, and inhibits tumor regeneration in BCSCs Breast cancer Phase I NCT00645333 (March 27, 2008) Well tolerated, but exists dose-limiting toxicity (DLT) [58]
PF-03084014 γ-secretase Inhibits CSC self-renewal and proliferation, and induces CSCs differentiation HCC Preclinical August, 2017 Induces gastrointestinal toxicity and exists DLT [59]
N1ICD, Hes-1, and Hey-1 Decreases CD44+/CD24− and ALDH+ population Pancreatic cancer Phase II NCT02109445(April 9, 2014)
Notch Diminishes CD133+/CD44+ and ALDH+ subpopulations and eliminates CSCs Breast cancer Phase I NCT01876251(June 12, 2013)
RO4929097 γ-secretase Combined with 5-FU can decrease the proportion of CSC subgroup INS Preclinical February, 2018 Fatigue is the most common toxicities, but it has DLT [60]
DAPT Notch1 Inhibits the proliferation of LSCs and regulates LSC self-renewal Leukemia Preclinical December, 2006 Induces low toxicity in cell and mice [61]
Inhibits the self-renewal ability of ovarian CSCs and the expression of stem markers Ovarian cancer Preclinical June, 2011
Quinomycin A Notch ligands Inhibits pancreatic cancer microsphere formation, the stem marker and the number of CSCs Pancreatic cancer Preclinical January 19, 2016 Induces gastrointestinal toxicity [62]