TL02-59 dihydrochloride
作者：齊岳
發布時間：2023-08-25
09:10:33
點擊數：
產品名稱：TL02-59 dihydrochloride
產品描述：
| 產品描述 | TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM). |
| 靶點活性 | Fgr:0.03 nM , Hck:160 nM , Lyn:0.1 nM |
| 體外活性 | 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. |
| 體內活性 | 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 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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