2407610-46-0

2407610-46-0 structure
2407610-46-0 structure
  • Name: PTPN2/1-IN-1
  • Chemical Name: PTPN2/1-IN-1
  • CAS Number: 2407610-46-0
  • Molecular Formula: C13H11FN2O5S
  • Molecular Weight: 326.30
  • Create Date: 2023-09-25 07:54:22
  • Modify Date: 2026-06-30 10:49:47
  • 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].

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

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

Molecular Formula C13H11FN2O5S
Molecular Weight 326.30
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