| Description | Sirpiglenastat (DRP-104) is a glutamine antagonist, a prodrug of DON, with antitumor activity that acts by inhibiting glutamine metabolism and stimulating the innate and adaptive immune system. |
| In vitro | Treatment with Sirpiglenastat (DRP-104) exhibits broad immune cell modulation effects, including an increase in T cells, NK cells, and macrophages. Sirpiglenastat also reduces the levels of pro-tumorigenic cytokines such as VEGF and KC (IL-8)[1]. |
| In vivo | In CT26 bearing mice, treatment with Sirpiglenastat (DRP-104) at a dose of 0.5 mg/kg through subcutaneous injection once a day for 5 days results in a 90% inhibition of tumor growth by day 12, with a median survival of 36 days[1].Additionally, Sirpiglenastat treatment (0.5 mg/kg; s.c) significantly inhibits tumor growth in the H22 model[1]. |
| Synonyms | DRP-104 |
| molecular weight | 441.48 |
| Molecular formula | C22H27N5O5 |
| CAS | 2079939-05-0 |
| Storage | keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (181.21 mM), Sonication is recommended. |
| References | 1. 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. 2. 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. |