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Sirpiglenastat

Chemical Structure : Sirpiglenastat

CAS No.: 2079939-05-0

Sirpiglenastat (DRP-104, DRP104)

Catalog No.: PC-38422Not For Human Use, Lab Use Only.

DRP-104 (Sirpiglenastat) is a novel broad acting glutamine antagonist, has significant anticancer activity by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.

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Biological Activity

DRP-104 (Sirpiglenastat) is a novel broad acting glutamine antagonist, has significant anticancer activity by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DRP-104 (Sirpiglenastat) has significant single agent activity in various tumor types, including KEAP1 and STK11 mutant non-small cell lung cancers (NSCLC), osimertinib resistant NSCLC as well as PIK3CA/PTEN mutant head and neck squamous cell carcinoma (SCCHN).
DRP-104 mediated tumor growth inhibition (TGI) is associated with increased tumor-infiltrating leukocytes (TIL) including T, NKT, and NK cells; M1-polarized tumor associated macrophages; and decreased immune-suppressive cells such as MDSCs.

Physicochemical Properties

M.Wt 441.488
Formula C22H27N5O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

isopropyl (S)-2-((S)-2-acetamido-3-(1H-indol-3-yl)propanamido)-6-diazo-5-oxohexanoate

References

1. Yumi Yokoyama, et al. Cancer Res (2021) 81 (13_Supplement): 1563.

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