Formulation: A solid
Formal Name: 7-fluoro-2-(((5-methoxy-1H-imidazo[4,5-b]pyridin-2-yl)thio)methyl)quinazolin-4(3H)-one
Purity: ≥98%
Formula Markup: C16H12FN5O2S
Formula Weight: 357,4
Shelf life (days): 730
Notes: ENPP1 inhibitor 4e is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1; IC50 = 0.188 µM), an enzyme that degrades the stimulator of interferon genes (STING) activator 2'3'-cGAMP (Item No. 19887).{69139} It inhibits ENPP1 in MDA-MB-231 cells, which highly express ENPP1 (IC50 = 0.732 µM). ENPP1 inhibitor 4e is selectively cytotoxic to 4T1 murine metastatic breast cancer cells (IC50 = 2.99 µM) over non-cancerous L-02 and 293T cells at 50 µM. It increases serum levels of IFN-β in mice when administered at a dose of 0.5 mg/kg in combination with cGAMP when compared to mice administered only cGAMP or mice not receiving either compound, indicating that ENPP1 inhibitor 4e reduces the degradation of cGAMP.
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