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HPK1-IN-2 dihydrochloride 是一种高效的口服活性HPK1抑制剂,IC50小于0.05 µΜ,显示出抗肿瘤活性。此化合物还能够抑制Lck和Flt3激酶的活性,其IC50亦小于0.05 µΜ。
HPK1-IN-2 dihydrochloride 是一种高效的口服活性HPK1抑制剂,IC50小于0.05 µΜ,显示出抗肿瘤活性。此化合物还能够抑制Lck和Flt3激酶的活性,其IC50亦小于0.05 µΜ。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 8-10周 | |
50 mg | 询价 | 8-10周 |
产品描述 | HPK1-IN-2 dihydrochloride, a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1) with an IC 50 of less than 0.05 µM, demonstrates significant antitumor activity. It additionally exhibits inhibition of Lck kinase activity, with an IC 50 ranging from 0.05 to less than 0.5 µM, and Flt3 kinase activity, with an IC 50 of less than 0.05 µM [1]. |
体外活性 | In a-CD3-stimulated Jurkat E6.1 cells, HPK1-IN-2 (example A1) suppresses the phosphorylation of SLP76 at serine 376 and ERK1/2 at T202/Y204, achieving IC50 values of 0.3-1 µM and >3µM, respectively [1]. |
体内活性 | Treatment with HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) demonstrates a dose-dependent inhibition of tumor growth. Specifically, a daily dose of 75 mg/kg and 150 mg/kg achieved tumor growth reductions of 44% and 64%, respectively [1]. |
分子量 | 453.39 |
分子式 | C19H22Cl2N6OS |
CAS No. | 2375595-72-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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