Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1; IC50<0.05 μΜ). It also inhibits Lck (0.05 μΜ Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 25 mg/mL (55.14 mM),
Sonication is recommended.
You can also refer to dose conversion for different animals.
詳細
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HPK1-IN-2
2056122-11-1
Angiogenesis
Others
Tyrosine Kinase/Adaptors
FLT
Src
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 dihydrochloride
HPK-1-IN-2 dihydrochloride
HPK1IN2 dihydrochloride
Inhibitor
inhibitor
inhibit
説明
HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) 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.
ターゲット&IC50
FLT3:<0.05 µΜ , HPK1:IC50<0.05 µΜ, Lck:0.05 µΜ<IC50<0.5 µΜ
In vitro
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.
In vivo
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
保存条件
溶解度情報
参考文献
関連化合物ライブラリー
関連製品
投与量変換
In vivo投与量計算 (透明溶液)
計算器
技術サポート
Keywords