2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Polo-like Kinase (PLK) Apoptosis
  4. AAPK-25

AAPK-25 是一种有效选择性的 Aurora/PLK 激酶双重抑制剂，具有抗肿瘤活性。AAPK-25 可引起有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10 磷酸化反应，随后细胞凋亡激增。AAPK-25 靶向 Aurora-A, -B, -C 的 Kd 值为 23 nM-289 nM，靶向 PLK-1, -2, -3 的 Kd 值为 55-456 nM。

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AAPK-25 Chemical Structure

AAPK-25 Chemical Structure

CAS No. : 2247919-28-2

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规格 价格 是否有货 数量
5 mg ￥2242
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10 mg ￥3363
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Customer Review

AAPK-25 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM[1].

IC50 & Target

Kd: 23 nM (Aurora-A), 78 nM (Aurora-B), 289 nM (Aurora-C), 55 nM (PLK-1), 272 nM (PLK-2), 456 nM (PLK-3), 5.32 μM (ERK), 7.11 μM (PI3K), 8.02 μM (CDK)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
11.6 μM
Compound: AAPK-25
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
[PMID: 31381325]
Calu-6 IC50
5.3 μM
Compound: AAPK-25
Antiproliferative activity against human Calu6 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human Calu6 cells measured after 48 hrs by MTT assay
[PMID: 31381325]
HCT-116 IC50
0.4 μM
Compound: AAPK-25
Antiproliferative activity against human HCT116 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells measured after 48 hrs by MTT assay
[PMID: 31381325]
MCF7 IC50
2.3 μM
Compound: AAPK-25
Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
[PMID: 31381325]
体外研究
(In Vitro)

AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC50s of 0.4, 5.3, 11.6, and 2.3 μM, respectively[1].
AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line[1].
AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block[1].
AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways[1].

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

AAPK-25 相关抗体:
体内研究
(In Vivo)

AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model[1].

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

442.32

Formula

C21H13Cl2N3O2S
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (113.04 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 2.2608 mL 11.3040 mL 22.6081 mL
5 mM 0.4522 mL 2.2608 mL 4.5216 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 (protect from light)。-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

只
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

AAPK-25 相关分类

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 (protect from light)。-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 2.2608 mL 11.3040 mL 22.6081 mL 56.5202 mL
5 mM 0.4522 mL 2.2608 mL 4.5216 mL 11.3040 mL
10 mM 0.2261 mL 1.1304 mL 2.2608 mL 5.6520 mL
15 mM 0.1507 mL 0.7536 mL 1.5072 mL 3.7680 mL
20 mM 0.1130 mL 0.5652 mL 1.1304 mL 2.8260 mL
25 mM 0.0904 mL 0.4522 mL 0.9043 mL 2.2608 mL
30 mM 0.0754 mL 0.3768 mL 0.7536 mL 1.8840 mL
40 mM 0.0565 mL 0.2826 mL 0.5652 mL 1.4130 mL
50 mM 0.0452 mL 0.2261 mL 0.4522 mL 1.1304 mL
60 mM 0.0377 mL 0.1884 mL 0.3768 mL 0.9420 mL
80 mM 0.0283 mL 0.1413 mL 0.2826 mL 0.7065 mL
100 mM 0.0226 mL 0.1130 mL 0.2261 mL 0.5652 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:

AAPK-252247919-28-2AAPK25AAPK 25Aurora KinasePolo-like Kinase (PLK)ApoptosisInhibitorinhibitorinhibit

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目录号：
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