For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I036307 |
| CAS Number | 2079939-05-0 |
| Synonyms | propan-2-yl (2S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-6-diazo-5-oxohexanoate |
| Molecular Formula | C22H27N5O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H27N5O5/c1-13(2)32-22(31)19(9-8-16(29)12-25-23)27-21(30)20(26-14(3)28)10-15-11-24-18-7-5-4-6-17(15)18/h4-7,11-13,19-20,24H,8-10H2,1-3H3,(H,26,28)(H,27,30)/t19-,20-/m0/s1 |
| InChIKey | LQNMCWOJACNQQM-PMACEKPBSA-N |
| SMILES | CC(C)OC(=O)C(CCC(=O)C=[N+]=[N-])NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C |
| Reference | [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. [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. |
