Formulation: A solid
Formal Name: 1-hydroxy-2-(2-propen-1-yl)-9,10-anthracenedione
Purity: ≥98%
Formula Markup: C17H12O3
Formula Weight: 264,3
Shelf life (days): 1460
CAS Number: 64302-87-0
Notes: R162 is an inhibitor of glutamate dehydrogenase 1 (GDH1; IC50 = 23 µM).{64361} It decreases intracellular fumarate levels and increases the production of mitochondrial reactive oxygen species (ROS) in human H1299 lung and MDA-MB-231 breast cancer cells. R162 (10-40 µM) inhibits proliferation in a panel of human cancer cell lines, including lung, breast, and leukemia cells, but not normal human HaCaT keratinocytes, MRC-5 lung fibroblasts, or foreskin fibroblasts. It reduces tumor growth and intratumoral GDH1 activity in an H1299 mouse xenograft model when administered at a dose of 20 mg/kg. R162 also reduces liver metastasis in a liver kinase B1-deficient lung cancer patient-derived xenograft (PDX) mouse model when administered at the same dose.{64362}
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