AAPK-25|cas:2247919-28-2|西域试剂

AAPK-25,98.31%

产品编号：Bellancom-126249| CAS NO：2247919-28-2| 分子式：C₂₁H₁₃Cl₂N₃O₂S| 分子量：442.32

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-126249	￥2900.00	杭州北京（现货）
Bellancom-126249	￥4300.00	杭州北京（现货）
Bellancom-126249	￥7800.00	杭州北京（现货）
Bellancom-126249	￥11800.00	杭州北京（现货）

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AAPK-25

产品介绍

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 H3^Ser10 磷酸化反应，随后细胞凋亡激增。AAPK-25 靶向 Aurora-A, -B, -C 的 K_d 值为 23 nM-289 nM，靶向 PLK-1, -2, -3 的 K_d 值为 55-456 nM。

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 H3^Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with K_d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K_d values ranging from 55-456 nM.

体外研究

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.
AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line.
AAPK-25 has significantly increased histone H3^Ser10 phosphorylation, indicating a markedly mitotic block.
AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways.

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

体内研究

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

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

体内研究

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

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (113.04 mM; Need ultrasonic)

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
10 mM	0.2261 mL	1.1304 mL	2.2608 mL

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。

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)

参考文献