Sirpiglenastat  (Synonyms: DRP-104)

Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response^[1][2].

Sirpiglenastat (DRP-104) treatment shows broad immune cell modulation effects including increased T, NK, and macrophages. Sirpiglenastat decreases pro-tumorigenic cytokines such as VEGF and KC (IL-8)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CT26 bearing mice treated with Sirpiglenastat (DRP-104) (0.5 mg/kg; s.c.; once a day; for 5 days) shows tumor growth inhibition at day 12 of 90%. Median survival days are 36 days^[1].
Sirpiglenastat (0.5 mg/kg; s.c) treatment significantly inhibits tumor growth in the H22 model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

441.48

C₂₂H₂₇N₅O₅

2079939-05-0

Solid

Off-white to yellow

CC(C)OC([C@H](CCC(C=[N+]=[N-])=O)NC([C@@H](NC(C)=O)CC1=CNC2=CC=CC=C12)=O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Yumi Yokoyama, et al. DRP-104, a novel broad acting glutamine antagonist, induces distinctive immune modulation mechanisms and synergistic efficacy in combination with immune checkpoint blockade. J Immunother Cancer. 2019 Nov 6;7(Suppl 1):282.  [Content Brief]

  [2]. Yumi Yokoyama, et al. DRP-104, a broad acting glutamine antagonist, synergizes with immune checkpoint blockade in vivo. Cancer Res 2021;81(13_Suppl):Abstract nr 1563.