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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
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $71 | In Stock | |
5 mg | $146 | In Stock | |
10 mg | $243 | In Stock | |
25 mg | $406 | In Stock | |
50 mg | $577 | In Stock | |
100 mg | $768 | In Stock | |
200 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $173 | In Stock |
Description | 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 |
Targets&IC50 | FLT3:<0.05 µΜ , HPK1:IC50<0.05 µΜ, Lck:0.05 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 |
Alias | 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 |
Molecular Weight | 380.47 |
Formula | C19H20N6OS |
Cas No. | 2056122-11-1 |
Smiles | NC1=C(C=2NC=3C(N2)=CC=C(C3)N4CCN(C)CC4)C(=O)NC5=C1C=CS5 |
Relative Density. | 1.418 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | H2O: 25 mg/mL (55.14 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
H2O
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