AKN-028 acetate|西域试剂

AKN-028 acetate,99.95%

产品编号：Bellancom-118304B| 分子式：C₁₉H₁₈N₆O₂| 分子量：362.39

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货号	价格	库存与货期
Bellancom-118304B	￥900.00	杭州北京（现货）
Bellancom-118304B	￥1530.00	杭州北京（现货）
Bellancom-118304B	￥3150.00	杭州北京（现货）
Bellancom-118304B	￥4950.00	杭州北京（现货）
Bellancom-118304B	￥8550.00	杭州北京（现货）

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AKN-028 acetate

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 novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀ value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC₅₀=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

体外研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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