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Sirpiglenastat is a prodrug form of the glutaminase inhibitor 6-diazo-5-oxo-L-nor-leucine (DON; Item No. 17580).1 Sirpiglenastat decreases P493B lymphoma cell viability (EC50 = 10 µM). In vivo, sirpiglenastat is metabolized to DON in tumor tissues, but metabolized to an inactive metabolite in gastrointestinal tissues, in EL4 murine T cell lymphoma, or MC-38 murine colon, EO771 murine breast, or 3LL Lewis lung carcinoma tumor-bearing CES1-/- mice, a model designed to more closely mimic human metabolism. It reduces tumor size in EL4 tumor-bearing CES1-/- mice when administered at doses of 0.1, 0.3, and 1 mg/kg.
WARNING This product is not for human or veterinary use.
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