Formulation: A solid
Formal Name: (2Z)-3-fluoro-4-(8-quinolinylsulfonyl)-2-buten-1-amine, dihydrochloride
Purity: ≥98%
Formula Markup: C13H13FN2O2S • 2HCl
Formula Weight: 353,2
Shelf life (days): 1460
CAS Number: 2409964-23-2
Notes: PXS-5505 is a pan inhibitor of lysyl oxidase (LOX) and LOX-like oxidases (LOXL; IC50s = 0.493, 0.159, 0.57, 0.18, and 0.19 µM for fibroblast LOX and recombinant human LOXL1-4, respectively).{69837} It is selective for LOX and LOXL1-4 over other recombinant human oxidases, including diamine oxidase (DAO), vascular adhesion protein-1 (VAP-1), monoamine oxidase A (MAO-A), and MAO-B (IC50s = >30 µM for all). PXS-5505 (15 mg/kg) reduces bleomycin-induced increases in dermal thickness and the levels of α-smooth muscle actin in a mouse model of systemic sclerosis.{69838} It reduces fibrosis in rodent models of bleomycin-induced pulmonary fibrosis, cardiac ischemia-reperfusion injury, renal unilateral ureteral obstruction, and carbon tetrachloride-induced liver fibrosis. It also reduces collagen crosslinking in KPC cancer-associated fibroblast (CAF) 3D organotypic matrices.{69837} PXS-5505 (20 mg/kg) increases survival to a greater extent than gemcitabine alone when administered in combination with the anticancer nucleoside derivative gemcitabine (Item Nos. 11690 / 9003096), reduces gemcitabine-induced increases in collagen levels and stiffness, and reduces liver metastatic burden in autochthonous KPC pancreatic ductal adenocarcinoma mouse models.
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