| Identification | Back Directory | [Name]
L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester | [CAS]
2079939-05-0 | [Synonyms]
Sirpiglenastat
L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester | [Molecular Formula]
C22H27N5O5 | [MOL File]
2079939-05-0.mol | [Molecular Weight]
441.49 |
| Chemical Properties | Back Directory | [solubility ]
DMSO: Sparingly Soluble: 1-10 mg/mL | [form ]
Solid | [color ]
Off-white to yellow | [InChIKey]
LQNMCWOJACNQQM-XEBFJNFFNA-N | [SMILES]
C(C1=CNC2=CC=CC=C12)[C@H](NC(=O)C)C(=O)N[C@@H](CCC(=O)C=[N+]=[N-])C(=O)OC(C)C |&1:10,18,r| |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | Animal Model: | CT26 bearing mice[1] | | Dosage: | 0.5 mg/kg
| | Administration: | s.c.; once a day; for 5 days | | Result: | Showed tumor growth inhibition in mice. |
| [References]
[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. DOI:10.1186/s40425-019-0763-1
[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. |
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