LW106 IDO1 inhibitor RGNCY-0114
Per 10 mg
LW106 is a novel idoleamine 2.3-dioxygenase 1 (IDO1) inhibitor. IDO1 is emerging as an important new target for the treatment of malignant tumors that are characterized by disregulated tryptophan metabolism. LW106 was shown to dose-dependently inhibit the outgrowth of xenograft tumors that were incoluated in immunocompetent C57BL6 mice but not nude mice or Ido-/- mice with a stronger antitumor efficacy than epacadostat (an existing IDO1 inhibitor). LW106 also increased intratumoral infiltration of proliferative Teff cells and reduced recruitment of proiferative Treg cells and non-hematopoietic cells. LW106 treatment resulted in a reduced subpopulation of cancer stem cells in xenigrafted tmors where fewer proliferative and invasive tumor cells and more apoptotic tumor cells were observed. IDO1 IC50 = 1.57 µM.
Systematic Name: (E)-(4-amino-1,2,5-oxadiazol-3-yl)(isoindolin-2-yl)methanone oxime
Mol Wt: 245.24
LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour microenvironment. Rong Fu et al. British Journal of Pharmacology (2018) 175 3034–3049.
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