AAPK-25

立即咨询

AAPK-25

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2247919-28-2

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 selectiveAurora/PLKdual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3^Ser10phosphorylation and followed by a surge inapoptosis. AAPK-25 targets Aurora-A, -B, and -C withK_dvalues ranging from 23-289 nM, as well as PLK-1, -2, and -3 withK_dvalues 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]

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 H3^Ser10phosphorylation, 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].

体内研究
(In Vivo)

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

分子量

442.32

性状

Solid

Formula

C₂₁H₁₃Cl₂N₃O₂S

CAS 号

2247919-28-2

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

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。