HPK1-IN-2 是一种有效且具有口服活性的造血祖细胞激酶-1 抑制剂(HPK1;IC50<0.05 μM)。它还抑制 Lck (0.05 μM
产品描述
HPK1-IN-2 dihydrochloride is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1;IC50<0.05 μΜ). It also inhibits Lck (0.05 μΜ
体外活性
In a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 μΜ and >3μΜ, respectively.
体内活性
HPK1-IN-2 (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
Cas No.
2056122-11-1
分子式
C19H20N6OS
分子量
380.47
别名
Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2;HPK1-IN-2
储存和溶解度
H2O:25 mg/mL (55.14 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years