2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Apoptosis Caspase
  4. AKN-028

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。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 AKN-028 acetate 通常具有更好的水溶性和稳定性。

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AKN-028 Chemical Structure

AKN-028 Chemical Structure

CAS No. : 1175017-90-9

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AKN-028 的其他形式现货产品:

Customer Review

Other Forms of AKN-028:

AKN-028 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AKN-028, 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 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 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].

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

AKN-028 相关抗体:

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].

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

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
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.
纯度 & 产品资料
参考文献

AKN-028 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AKN-0281175017-90-9AKN028AKN 028FLT3ApoptosisCaspaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3FLT3 autophosphorylationacute myeloid leukemiacytotoxicAML cell linesInhibitorinhibitorinhibit

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产品名称：
AKN-028
目录号：
HY-118304
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