L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester
- Product Name
- L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester
- CAS No.
- 2079939-05-0
- Chemical Name
- L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester
- Synonyms
- Sirpiglenastat;L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester;isopropyl (S)-2-((S)-2-acetamido-3-(1H-indol-3-yl)propanamido)-6-diazo-5-oxohexanoate
- CBNumber
- CB911094589
- Molecular Formula
- C22H27N5O5
- Formula Weight
- 441.49
- MOL File
- 2079939-05-0.mol
L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester Property
- 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|
L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester Chemical Properties,Usage,Production
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.
[3] RANA RAIS. Discovery of DRP-104, a tumor-targeted metabolic inhibitor prodrug[J]. Science Advances, 2022, 8 46. DOI: 10.1126/sciadv.abq5925
L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester Preparation Products And Raw materials
Raw materials
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L-Norleucine, N-acetyl-L-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester Suppliers
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