中文名称: | AAPK-25 | ||||
---|---|---|---|---|---|
英文名称: | AAPK-25 | ||||
别名: | AAPK-25 | ||||
CAS No: | 2247919-28-2 | 分子式: | C21H13Cl2N3O2S | 分子量: | 442.32 |
CAS No: | 2247919-28-2 | ||||
分子式: | C21H13Cl2N3O2S | ||||
分子量: | 442.32 |
包装规格:
5mg 10mg 25mg 50mg in glass bottle
产品简介:
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。
溶解性:
溶于DMSO(50mg/ml)
储备液保存:
-80°C, 6 months
-20°C, 1 month
(protect from light)
-20°C, 1 month
(protect from light)
靶点:
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)
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:
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 H3Ser10 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.
AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line.
AAPK-25 has significantly increased histone H3Ser10 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.
体内研究:
AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model.
保存条件:
2-8°C 避光
注意事项:
1、为了您的安全和健康,请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献
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