AKN-028

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AKN-028

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。

CAS NO:

1175017-90-9

AKN-028 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 抑制 FLT3 自磷酸化。AKN-028 诱导剂量依赖性的细胞毒性反应 (平均IC₅₀=1 μM)。AKN-028 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 可用于急性髓系白血病 (AML) 的研究。

生物活性

AKN-028, a noveltyrosine kinase (TK)inhibitor, is a potent, orally activeFMS-like receptor tyrosine kinase 3 (FLT3)inhibitor with anIC₅₀value of 6 nM. AKN-028 inhibitsFLT3autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (meanIC₅₀=1 μM). AKN-028 inducesapoptosisby activation ofcaspase 3. AKN-028 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) inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner^[1].
AKN-028 (10 μM; 72 h; tumor cell lines) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11^[1].

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.

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).

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) 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

302.33

Formula

C₁₇H₁₄N₆

CAS 号

1175017-90-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : 125 mg/mL(413.46 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.3076 mL	16.5382 mL	33.0764 mL
5 mM	0.6615 mL	3.3076 mL	6.6153 mL
10 mM	0.3308 mL	1.6538 mL	3.3076 mL