HPK1-IN-2 dihydrochloride

• CAT Number: I040085
• CAS Number: 2375595-72-3
• Molecular Formula: C19H22Cl2N6OS
• Molecular Weight: 453.39
• Purity: ≥95%
• Synonyms: 4-amino-5-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-7H-thieno[2,3-b]pyridin-6-one;dihydrochloride
• InChI: InChI=1S/C19H20N6OS.2ClH/c1-24-5-7-25(8-6-24)11-2-3-13-14(10-11)22-17(21-13)15-16(20)12-4-9-27-19(12)23-18(15)26;;/h2-4,9-10H,5-8H2,1H3,(H,21,22)(H3,20,23,26);2*1H
• InChIKey: XESGZTINOLHKPH-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(NC4=O)SC=C5)N.Cl.Cl

HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 µΜIn a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 (example A1) inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 µΜ and >3µΜ, respectively[1].
HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) treatment shows a dose-dependently tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumour growth by 44% and 64%, respectively[1].

Reference

[1]. Peter Brent Sampson, et al. Hpk1 inhibitors and methods of using same. WO2016205942A1.