Tegeprotafib( —— )

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

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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

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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

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Pathway

Metabolic Enzyme/Protease
Target

Phosphatase
Recptor

Phosphatase
Research Area

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Indication

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

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