Home>>Signaling Pathways>> Cell Cycle/Checkpoint>> PLK>>Ro3280

Ro3280 Sale

目录号 : GC13903

A selective Plk1 inhibitor

Ro3280 Chemical Structure

Cas No.:1062243-51-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,890.00
现货
5mg
¥1,365.00
现货
50mg
¥7,256.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment:

Leukemia cells or primary leukemia cells (2 × 104) are seeded in 96-well plates overnight and incubated with DMSO, or increasing concentrations of RO3280 (0.05-120 μM) for 24 h. The same volume of DMSO added to the vehicle treated wells. Each drug concentration is replicated four times. Then, 10 μL CCK8 solution is added to each well, incubated at 37°C for 2-4 h and the optical density (OD) values are measured at 450 nm using a scanning multi-well spectrophotometer. Relative survival rate is calculated from the absorbance values compared with the control group. The proliferation of cells is calculated as a percentage of the DMSO-treated control wells with 50% inhibitory concentration (IC50) values derived after plotting proliferation values on a logarithmic curve. The IC50 of PLK1 inhibitor is calculated by Graph Prism software[1].

Animal experiment:

Briefly, mice (female, 4-5 weeks of age) are used in the assay. Cells (5 × 106 cells in 150 μL) are suspended in RPMI 1640 and injected subcutaneously into the flank of each BALB/c nude mouse. On day 5, tumour size is measured, the animals are randomized into two groups (n = 15 per group), and RO3280 (40 mg/kg, once every 5 days) treatment is initiated by intraperitoneal injection. The control group is treated with vehicle (1.5% DMSO in PBS). The drug (or vehicle) treatment is performed for 40 days. The length and width of the resulting tumours (in millimetres) are measured every 3 days with callipers. The tumour diameter is measured, and the volume (length × width2 × 0.52) is calculated. The mice are humanely killed on day 45, and the tumours are dissected and weighed. Western blot and immunohistochemistry assays are also performed with these sections. Then, the tumours are fixed, embedded and cut into 3‐μm‐thick sections, which are subsequently stained with haematoxylin and eosin to permit the observation of the tumour margin[3].

References:

[1]. Wang NN, et al. Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
[2]. Chen S, et al. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50.
[3]. Zhang Z, et al. Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. J Cell Mol Med. 2017 Apr;21(4):758-767.

产品描述

Ro3280 is a selective inhibitor of PLK1 with IC50 value of 3 nM [1].

Polo-like kinase 1 (PLK1) is an enzyme and plays an important role in regulating cell cycles as an early trigger for G2/M phase transition. It has been shown that PLK1 is over-expressed in a variety of cancer cells and thus is regarded as a promising target for cancer drugs [2].

When tested with a panel of acute leukemia cell lines, Ro3280 showed inhibitory function on U937, HL 60, NB4, K562, MV4-11, and CCRF with IC50 value of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM, and 162 nM, respectively. It was interesting to notice that ALL cells (35.49-110.76 nM) were more sensitive to Ro3280 compared with AML cells (IC50, 52.80-147.50 nM). Further, it was showed that Ro3280 treatment decreased cell viability, induced apoptosis and disrupted cell cycle [3]. In H82 (lung cancer), HT-29 (colon cancer), MDA-MB-468 (breast cancer), PC3 (prostate cancer), and A375 (cutaneum carcinoma), Ro3280 treatment inhibited PLK1 with the IC50 was 5 nM, 10 nM, 19 nM, 12 nM, and 70 nM, respectively [1].

In nude mice model with HT-29 cells subcutaneous xenograft, administration of Ro3280 caused significant anti-tumor activity with 78% reduction at the dose of 40 mg/kg, once a week and then completely regressed tumor when more drug and more frequent [1].

References:
[1].  Chen, S., et al., Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett, 2012. 22(2): p. 1247-50.
[2].  Czaplinski, S., et al., Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget, 2015.
[3].  Wang, N.N., et al., Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci, 2015. 16(1): p. 1266-92.

Chemical Properties

Cas No. 1062243-51-9 SDF
化学名 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Canonical SMILES CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC
分子式 C27H35F2N7O3 分子量 543.61
溶解度 ≥ 27.2mg/mL in DMSO 储存条件 Store at -20°C
General tips 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.8396 mL 9.1978 mL 18.3955 mL
5 mM 0.3679 mL 1.8396 mL 3.6791 mL
10 mM 0.184 mL 0.9198 mL 1.8396 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置