产品
编 号:F752079
分子式:C13H11FN2O5S
分子量:326.3
产品类型
结构图
CAS No: 2407610-46-0
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产品详情
生物活性:
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.
体内研究:
Tegeprotafib (Compound 124; 300 mg/kg; oral; BID for 21 days) 在小鼠中具有抗肿瘤活性。Animal Model:Female C57B1/6 mice, MC-38 tumor model
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.
体外研究:
Tegeprotafib (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%。