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Sirpiglenastat

CAS No. 2079939-05-0

Sirpiglenastat( —— )

Catalog No. M35655 CAS No. 2079939-05-0

Sirpiglenastat (DRP-104), a glutamine antagonist and prodrug of DON, exhibits antitumor activity by inhibiting glutamine metabolism and stimulating both the innate and adaptive immune systems.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Sirpiglenastat
  • Note
    Research use only, not for human use.
  • Brief Description
    Sirpiglenastat (DRP-104), a glutamine antagonist and prodrug of DON, exhibits antitumor activity by inhibiting glutamine metabolism and stimulating both the innate and adaptive immune systems.
  • Description
    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.
  • In Vitro
    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).
  • 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. Sirpiglenastat (0.5 mg/kg; s.c) treatment significantly inhibits tumor growth in the H22 model.Animal Model:CT26 bearing mice Dosage:0.5 mg/kg Administration:s.c.; once a day; for 5 days Result:Showed tumor growth inhibition in mice.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Glutaminase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2079939-05-0
  • Formula Weight
    441.48
  • Molecular Formula
    C22H27N5O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (226.51 mM; Ultrasonic )
  • SMILES
    C([C@@H](C(N[C@H](C(OC(C)C)=O)CCC(C=[N+]=[N-])=O)=O)NC(C)=O)C=1C=2C(NC1)=CC=CC2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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.?
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