Bioactivity | 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]. |
Target | IC50: 4.4 nM (PTPN2), 1-10 nM (PTP1B) |
Invitro | 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: |
Name | PTPN2/1-IN-1 |
CAS | 2407610-46-0 |
Formula | C13H11FN2O5S |
Molar Mass | 326.30 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Elliot FARNEY, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. Patent WO2019246513A1. |