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AKN-028 acetate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AKN-028 acetate图片
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
AKN-028 acetate 是一种新型酪氨酸激酶 (TKI) 抑制剂，是一种有效的口服活性的 FMS 样受体酪氨酸激酶 3 (FLT3) 抑制剂，其IC50值为 6 nM。AKN-028 acetate 抑制 FLT3 自磷酸化。AKN-028 acetate 诱导剂量依赖性的细胞毒性反应 (平均IC50=1 μM)。AKN-028 acetate 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 acetate 可用于急性髓系白血病 (AML) 的研究。
生物活性

AKN-028 acetate, a noveltyrosine kinase (TK)inhibitor, is a potent, orally activeFMS-like receptor tyrosine kinase 3 (FLT3)inhibitor with anIC50value of 6 nM. AKN-028 acetate inhibitsFLT3autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (meanIC50=1 μM). AKN-028 acetate inducesapoptosisby activation ofcaspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML)[1].

IC50& Target

IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)[1]

体外研究
(In Vitro)

AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) acetate inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner[1].
AKN-028 (10 μM; 72 h; tumor cell lines) acetate is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1].

Cell Cytotoxicity Assay[1]

Cell Line:Tumor cell lines
Concentration:10 μM
Incubation Time:72 hours
Result:Had cytotoxic activity was highest in MV4-11 and MOLM-13 (IC50<50 nM), followed by the three other AML cell lines (IC50=0.5-6 μM).

Western Blot Analysis[1]

Cell Line:Mouse embryonal fibroblasts either overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryoblastic leukemia M07 cells overexpressing KIT
Concentration:0.1 nM-100 μM
Incubation Time:15 hours
Result:Inhibited FLT3 and KIT autophosphorylation.
体内研究
(In Vivo)

AKN-028 (15 mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) acetate inhibits growth of primary AML and MV4-11 cells in mice[1].

Animal Model:Male C57 black mice with MV4-11 xenografts[1]
Dosage:15 mg/kg
Administration:Subcutaneous injection; twice daily, for 6 days
Result:Inhibited tumor growth and did not affect body weight.
Clinical Trial
分子量

362.39

性状

Solid

Formula

C19H18N6O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)