Tegeprotafib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tegeprotafib (PTPN2/1-IN-1) 是一种具有口服活性的 PTPN1 和 PTPN2 抑制剂，对 PTPN2 和 PTP1B 的IC50 分别为 4.4 nM 和 1-10 nM。

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.

——

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.

——

Metabolic Enzyme/Protease

Phosphatase

Phosphatase

——

——

2407610-46-0

326.3

C13H11FN2O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (306.47 mM; 超声助溶 )

O=C1NS(=O)(=O)N(C=2C(O)=CC3=CC=C(OC)C=C3C2F)C1

——

(-20℃)

With Ice Pack

≥ 2 years