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

AKN-028 acetate 

目录号: HY-118304B 纯度: 99.95%
COA 产品使用指南

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。

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AKN-028 acetate Chemical Structure

AKN-028 acetate Chemical Structure

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Customer Review

Other Forms of AKN-028 acetate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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).

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 小时;小鼠胚胎成纤维细胞和人急性巨核细胞白血病 M07 细胞) 乙酸盐以剂量依赖性方式抑制 FLT3 和 KIT 自磷酸化[1]
AKN-028 (10 μM;72 小时;肿瘤细胞系) 醋酸盐对 AML 细胞系具有细胞毒性并诱导 AML 细胞系 MV4-11 发生细胞凋亡[1]

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

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 (15mg/kg;i.h.;每天两次,持续 6 天;具有 MV4-11 异种移植物的雄性 C57 黑鼠) 醋酸盐抑制小鼠原代 AML 和 MV4-11 细胞的生长[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

362.39

Formula

C19H18N6O2

性状

固体

颜色

Brown to orange

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (275.95 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 2.7595 mL 13.7973 mL 27.5946 mL
5 mM 0.5519 mL 2.7595 mL 5.5189 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

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

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7595 mL 13.7973 mL 27.5946 mL 68.9864 mL
5 mM 0.5519 mL 2.7595 mL 5.5189 mL 13.7973 mL
10 mM 0.2759 mL 1.3797 mL 2.7595 mL 6.8986 mL
15 mM 0.1840 mL 0.9198 mL 1.8396 mL 4.5991 mL
20 mM 0.1380 mL 0.6899 mL 1.3797 mL 3.4493 mL
25 mM 0.1104 mL 0.5519 mL 1.1038 mL 2.7595 mL
30 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2995 mL
40 mM 0.0690 mL 0.3449 mL 0.6899 mL 1.7247 mL
50 mM 0.0552 mL 0.2759 mL 0.5519 mL 1.3797 mL
60 mM 0.0460 mL 0.2300 mL 0.4599 mL 1.1498 mL
80 mM 0.0345 mL 0.1725 mL 0.3449 mL 0.8623 mL
100 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6899 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.

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产品名称:
AKN-028 acetate
目录号:
HY-118304B
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