HPK1-IN-2 dihydrochloride
產品名稱:HPK1-IN-2 dihydrochloride
產品描述:
產品描述 | 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<IC50<0.5 μΜ) and Flt3 (IC50<0.05 μΜ) kinase activities with antitumor activity |
靶點活性 | FLT3:<0.05 μΜ , HPK1:IC50<0.05 μΜ, Lck:0.05 μΜ<IC50<0.5 μΜ |
體外活性 | 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. |
體內活性 | 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 |
別名 | 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 |
分子量 | 380.47 |
分子式 | C19H20N6OS |
CAS No. | 2056122-11-1 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 25 mg/mL (55.14 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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