| Identification | Back Directory | [Name]
1,2,5-Thiadiazolidin-3-one, 5-(1-fluoro-3-hydroxy-7-methoxy-2-naphthalenyl)-, 1,1-dioxide | [CAS]
2407610-46-0 | [Synonyms]
Tegeprotafib
5-(1-fluoro-3-hydroxy-7-methoxy-2-naphthyl)-1,1-dioxo-1,2,5-thiadiazolidin-3-one
1,2,5-Thiadiazolidin-3-one, 5-(1-fluoro-3-hydroxy-7-methoxy-2-naphthalenyl)-, 1,1-dioxide | [Molecular Formula]
C13H11FN2O5S | [MOL File]
2407610-46-0.mol | [Molecular Weight]
326.3 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
Tegeprotafib (Compound 124; 300 mg/kg; oral; BID for 21 days) shows antitumor activity in mice[1]. | Animal Model: | Female C57B1/6 mice, MC-38 tumor model[1] | | Dosage: | 300 mg/kg/dose | | Administration: | Oral, twice a day (BID) at 7am and 5pm for 21 days | | Result: | 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. |
| [References]
[1] Elliot FARNEY, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. Patent WO2019246513A1. |
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