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AKN-028 是酪氨酸激酶 FLT3的抑制剂,可剂量依赖性的诱导 FLT3的自磷酸化。
AKN-028 是酪氨酸激酶 FLT3的抑制剂,可剂量依赖性的诱导 FLT3的自磷酸化。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 198 | 现货 | |
5 mg | ¥ 478 | 现货 | |
10 mg | ¥ 816 | 现货 | |
25 mg | ¥ 1,680 | 现货 | |
50 mg | ¥ 2,490 | 现货 | |
100 mg | ¥ 3,550 | 现货 | |
500 mg | 询价 | 现货 |
产品描述 | AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation. |
靶点活性 | FGFR2:1200 nM (IC50), CLK1:140 nM (IC50), FLT3:6 nM (IC50), VEGFR2:520 nM (IC50), RPS6KA:220 nM (IC50) |
体外活性 | AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3 [1] . AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11 [1] . Cell Cytotoxicity Assay [1] Cell Line: AML cell line MV4-11. Concentration: 10 μM. Incubation Time: 24 h. Result: Was cytotoxic to primary AML cells, irrespective of FLT3 mutation status and quantitative FLT3 expression. |
体内活性 | AKN-028 (15?mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models [1] . Animal Model: Mice based AML and MV4-11 cells [1] . Dosage: 15?mg/kg. Administration: Subcutaneously injection twice daily. Result: Inhibited net growth of one of the primary AML samples (UPN26) in vivo and furthermore reduced the tumor mass of MV4-11 cell line. |
分子量 | 302.33 |
分子式 | C17H14N6 |
CAS No. | 1175017-90-9 |
Smiles | N(C=1N=C(C=NC1N)C=2C=CN=CC2)C=3C=C4C(=CC3)NC=C4 |
密度 | 1.405 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 20 mg/mL 66.15 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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