JAK2 JH2 binder-1 (compound 11) is a potent and selective JAK2 JH2 binder, with a K d of 37.1 nM. JAK2 JH2 binder-1 has the potential for various myeloproliferative neoplasms research [1].
In Vivo, JAK2 JH2 binder-1 (25 mg/kg, i.v., 3 times per week for 3 weeks) shows significant antitumor activity in C.B-17 SCID-beige mouse xenograft model[1].
In Vitro, JAK2 JH2 binder-1 (20 μM, 1-48 hours) completely inhibits STAT5 phosphorylation, effective in both V617F and wild-type JAK2 expressing cells[1].
References:
[1]. Losi ME, et, al. Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands. J Med Chem. 2022 Jun 23;65(12):8380-8400.
In Vivo, JAK2 JH2 binder-1 (25 mg/kg, i.v., 3 times per week for 3 weeks) shows significant antitumor activity in C.B-17 SCID-beige mouse xenograft model[1].
In Vitro, JAK2 JH2 binder-1 (20 μM, 1-48 hours) completely inhibits STAT5 phosphorylation, effective in both V617F and wild-type JAK2 expressing cells[1].
References:
[1]. Losi ME, et, al. Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands. J Med Chem. 2022 Jun 23;65(12):8380-8400.