AAPK-25|2247919-28-2|-陌孚医药/Medlife

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AAPK-25

目录号: PL13929 纯度: ≥98%

CAS No. :2247919-28-2

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PL13929-50mg	50mg	¥14589.09	请登录
PL13929-100mg	100mg	询价	询价
PL13929-200mg	200mg	询价	询价

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中文名称	AAPK-25
英文名称	AAPK-25
英文别名	4-((6-Chloro-2-methoxyacridin-9-yl)methyl)-2-((4-(2-(dimethylamino)ethyl)piperazin-1-yl)methyl)phenol;AAPK-25
Cas No.	2247919-28-2
分子式	C₃₀H₃₅ClN₄O₂
分子量	519.08
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	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 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.
性状	Solid
IC50 & Target[1][2]	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)
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. AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line. AAPK-25 has significantly increased histone H3 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model. has not independently confirmed the accuracy of these methods. They are for reference only.
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	[1]. Qi B, et al. Discovery of inhibitors of Aurora/PLK targets as anti-cancer agents. J Med Chem. 2019 Aug 5.

溶解度数据	In Vitro: DMSO : 50 mg/mL (113.04 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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