HPK1-IN-2 TFA is an orally active HPK1 inhibitor ( IC50 < 0.05 µM) with antitumor activity. HPK1-IN-2 TFA inhibits the activity of Lck ( IC50 <0.05 µM) and Flt3 ( IC50 < 0.05 µM) kinases [1].
In Vivo, HPK1-IN-2 (example A1) (75-150 mg/kg; oral gavage; daily; for 21 days) TFA treatment showed dose-dependent tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumor growth by 44% and 64%, respectively[1].
In Vitro, HPK1-IN-2 (example A1) TFA suppresses SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 μM and > 3 μM, respectively, in α-CD3 stimulated Jurkat E6.1 cells[1].
References:
[1]. Peter Brent Sampson, et al. Hpk1 inhibitors and methods of using same. WO2016205942A1.
In Vivo, HPK1-IN-2 (example A1) (75-150 mg/kg; oral gavage; daily; for 21 days) TFA treatment showed dose-dependent tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumor growth by 44% and 64%, respectively[1].
In Vitro, HPK1-IN-2 (example A1) TFA suppresses SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 μM and > 3 μM, respectively, in α-CD3 stimulated Jurkat E6.1 cells[1].
References:
[1]. Peter Brent Sampson, et al. Hpk1 inhibitors and methods of using same. WO2016205942A1.