Tegeprotafib

CAS No. 2407610-46-0

Tegeprotafib( —— )

Catalog No. M37224 CAS No. 2407610-46-0

Tegeprotafib (PTPN2/1-IN-1, Compound 124) is an orally active inhibitor targeting both PTPN2 and PTPN1B, with potent IC50 values of 4.4 nM for PTPN2 and 1-10 nM for PTPN1B, respectively .

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Tegeprotafib
  • Note
    Research use only, not for human use.
  • Brief Description
    Tegeprotafib (PTPN2/1-IN-1, Compound 124) is an orally active inhibitor targeting both PTPN2 and PTPN1B, with potent IC50 values of 4.4 nM for PTPN2 and 1-10 nM for PTPN1B, respectively .
  • Description
    Tegeprotafib (PTPN2/1-IN-1) (Compound 124) is an orally active PTPN1 and PTPN2 inhibitor with IC50s of 4.4 nM and 1-10 nM against PTPN2 and PTP1B, respectively.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Female C57B1/6 mice, MC-38 tumor modelDosage:300 mg/kg/dose Administration:Oral, twice a day (BID) at 7am and 5pm for 21 daysResult:Within 7-10 days of treatment, apparent tumor stasis and shrinkage was observed. 50% of mice achieved complete cures, and an overall TGIMEX was 75%. The frequency of functional, granzyme B (GzB) producing cells within the cytotoxic CD8+ T population in the spleen was 2.9-fold increased over vehicle control treated animals. Increased IP10 levels in plasma.
  • Synonyms
    ——
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Phosphatase
  • Recptor
    Phosphatase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2407610-46-0
  • Formula Weight
    326.3
  • Molecular Formula
    C13H11FN2O5S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (306.47 mM; Ultrasonic )
  • SMILES
    O=C1NS(=O)(=O)N(C=2C(O)=CC3=CC=C(OC)C=C3C2F)C1
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Elliot FARNEY, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. Patent WO2019246513A1.
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