| Name | PTPN2/1-IN-1 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4.4 nM (PTPN2), 1-10 nM (PTP1B)[1] |
| In Vitro | PTPN2/1-IN-1 (Compound 124; 5 days) 抑制 IFNγ (0.5 ng/mL) 诱导的 B16F10 细胞生长,33 μM 的生长抑制率为 60-90%[1]。 |
| In Vivo | PTPN2/1-IN-1 (Compound 124; 300 mg/kg; oral; BID for 21 days) 在小鼠中具有抗肿瘤活性[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 |
| Molecular Formula | C13H11FN2O5S |
|---|---|
| Molecular Weight | 326.30 |