LY 345899 (C09-1142-982)

LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase ( MTHFD1 ; DC301 ) and MTHFD2 inbhibitor with IC 50 values of 96 nM and 663 nM, respectively and a K i of 18 nM for MTHFD1In VitroLY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria . LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis . MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoLY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SW620 or PDX-based BABL/c nude colorectal cancer (CRC) modelDosage: 5-10 mg/kg Administration: Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks Result: Displayed lower cell proliferation indices and higher cell apoptosis. Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice.IC50& Target:Ki: 18 nM (MTHFD1),IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2). Specification: 10mM in DMSO Molecular Formula: C20H21N7O7 Molecular Weight: 471.4