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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。
AAPK-25图片
CAS NO:2247919-28-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

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 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。
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 H3Ser10phosphorylation and followed by a surge inapoptosis. AAPK-25 targets Aurora-A, -B, and -C withKdvalues ranging from 23-289 nM, as well as PLK-1, -2, and -3 withKdvalues 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 H3Ser10phosphorylation, 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 mg5 mg10 mg
1 mM2.2608 mL11.3040 mL22.6081 mL
5 mM0.4522 mL2.2608 mL4.5216 mL
10 mM0.2261 mL1.1304 mL2.2608 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。