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BI 2536

现货
Catalog No.
A3965
ATP竞争性的Plk1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,250.00
Ship with 10-15 days
5mg
¥ 850.00
Ship with 10-15 days
10mg
¥ 1,500.00
Ship with 10-15 days
50mg
¥ 4,700.00
Ship with 10-15 days

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Background

BI 2536 is a potent, ATP-competitive, well tolerated and highly specific human polo-like kinase 1 (PLK1) inhibitor with IC value of 0.83 nM, which shows 1000-fold selectivity against other kinases [1].

BI 2536 has been demonstrated to suppress cell growth and colony formation, it has been shown to induce mitotic arrest at G2/M phase and apoptosis in human cervical adenocarcinoma cell line HeLa [2].

BI 2536 has shown to have the effect of inhibiting cell proliferation in more than 20 tumor cell lines with half maximal effective concentration (EC50) values ranging from 2–25 nM. In vivo, multiple studies in xenograft models of human carcinoma have shown the anti-tumor activity of BI 2536 when the drug was intravenously administered 1-2 times every week [1].

References:
[1] Schöffski P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70.
[2] Pezuk JA1, Brassesco MS, Oliveira JC, Morales AG, Montaldi AP, Sakamoto-Hojo ET, Scrideli CA, Tone LG. Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells. Clin Exp Med. 2013 Feb;13(1):75-80.

文献引用

1. Kaisari S, Shomer P, et al. "Role of Polo-like kinase 1 in the regulation of the action of p31(comet) in the disassembly of mitotic checkpoint complexes." Proc Natl Acad Sci U S A. 2019 Jun 11;116(24):11725-11730. PMID:31118282
2. Chen LL, Wang YB, et al. "Phosphoproteome-based kinase activity profiling reveals the critical role of MAP2K2 and PLK1 in neuronal autophagy." Autophagy. 2017;13(11):1969-1980. PMID:28933595

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt521.67
Cas No.755038-02-9
FormulaC28H39N7O3
SynonymsBI-2536;BI2536
Solubility≥13.04 mg/mL in DMSO, ≥92.4 mg/mL in EtOH with ultrasonic, <2.56 mg/mL in H2O
Chemical Name4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
SDFDownload SDF
Canonical SMILESCCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HeLa-S3细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1 μM;24 h

应用

BI 2536对癌细胞生长细胞周期的效应通过免疫荧光显微镜和流式细胞仪进行评估。BI2536引起HeLa细胞积累4N DNA含量,表明细胞周期阻滞在G2期或有丝分裂期。在BI 2536处理的培养HeLa细胞中,有丝分裂图片显示异常的有丝分裂,其EC50值与诱导G2/M期停滞的值非常接近。

动物实验[1]:

动物模型

植入HCT 116细胞的免疫缺陷nu/nu小鼠

剂量

40–50mg/kg,1或2次/周;静脉注射

应用

据报道,在不同的异种移植模型中,BI 2536具有很好的疗效。例如,在HCT 116结肠癌中,BI 2536每周2次给药显示完全肿瘤抑制,每周1次给药时T/C值为16%。在更严格的具有较大HCT 116肿瘤模型中,直到癌结节的中值达到500 mm3时才开始治疗,BI 2536五个周期的治疗诱导显著的肿瘤消退,而对照小鼠显示疾病的发展。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Steegmaier M, Hoffmann M, Baum A, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Current Biology, 2007, 17(4): 316-322.

生物活性

描述 BI2536是一个有效的Plk1抑制剂,IC50值为0.83 nM。
靶点 Plk1          
IC50 0.83 nM          

质量控制

化学结构

BI 2536

相关生物数据

BI 2536

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BI 2536

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BI 2536