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

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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.
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (413.46 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

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体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
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给药剂量

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动物的平均体重

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由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

AKN-028 相关分类

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3076 mL 16.5382 mL 33.0764 mL 82.6911 mL
5 mM 0.6615 mL 3.3076 mL 6.6153 mL 16.5382 mL
10 mM 0.3308 mL 1.6538 mL 3.3076 mL 8.2691 mL
15 mM 0.2205 mL 1.1025 mL 2.2051 mL 5.5127 mL
20 mM 0.1654 mL 0.8269 mL 1.6538 mL 4.1346 mL
25 mM 0.1323 mL 0.6615 mL 1.3231 mL 3.3076 mL
30 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7564 mL
40 mM 0.0827 mL 0.4135 mL 0.8269 mL 2.0673 mL
50 mM 0.0662 mL 0.3308 mL 0.6615 mL 1.6538 mL
60 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3782 mL
80 mM 0.0413 mL 0.2067 mL 0.4135 mL 1.0336 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8269 mL
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：
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目录号：
HY-118304
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