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TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).
TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 5,400 | 35日内发货 | |
50 mg | ¥ 22,600 | 35日内发货 |
产品描述 | TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM). |
靶点活性 | Lyn:0.1 nM , Hck:160 nM , FGR:0.03 nM |
体外活性 | in TF-1 cells, TL02-59 dihydrochloride (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation , with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. |
体内活性 | TL02-59 (oral; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement. |
分子量 | 682.56 |
分子式 | C32H36Cl2F3N5O4 |
CAS No. | 2415263-06-6 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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