2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. Ro3280

Ro3280 是一种有效的，高度选择性的 PLK1 抑制剂，IC50 和 Kd 值分别为 3 nM 和 0.09 nM，对 PLK2 和 PLK3 几乎没作用。

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Ro3280

Ro3280 Chemical Structure

CAS No. : 1062243-51-9

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规格 价格 是否有货 数量
1 mg ￥766
In-stock
2 mg ￥1100
In-stock
5 mg ￥1600
In-stock
10 mg ￥2600
In-stock
25 mg ￥4488
In-stock
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Ro3280 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.

IC50 & Target[2]

PLK1

0.09 nM (Kd)

ALK

230 nM (Kd)

CAMKK1

1100 nM (Kd)

CAMKK2

87 nM (Kd)

DAPK1

100 nM (Kd)

DAPK3

70 nM (Kd)

FER

53 nM (Kd)

GAK

87 nM (Kd)

MYLK

170 nM (Kd)

PTK2

84 nM (Kd)

PTK2B

130 nM (Kd)

RPS6KA6 (KinDom.2)

560 nM (Kd)

TTK

51 nM (Kd)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T IC50
2.6 nM
Compound: Ro3280
Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
[PMID: 34710325]
HT-29 EC50
5 nM
Compound: 11
Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay
Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay
[PMID: 23664874]
MM1.S IC50
5.7 nM
Compound: Ro3280
Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
[PMID: 34710325]
体外研究
(In Vitro)

Ro3280 (RO3280) 抑制 NB4 和 K562 细胞中的 PLK1 活性，IC50 分别为 13.45 nM 和 301 nM。RO3280 对 6 种白血病细胞的生长具有抑制活性，对 U937、HL60、NB4、K562、分别为 MV4-11 和 CCRF 细胞系。RO3280 还抑制原代 ALL 和 AML 细胞的生长，IC50 分别为 35.49-110.76 nM 和 52.80-147.50 nM。RO3280 (50 或 100 nM) 诱导急性白血病细胞凋亡和细胞周期紊乱[1]。
Ro3280 在 H82、H69、A549 肺癌细胞系中表现出强大的活性，EC50 分别为 6 nM、7 nM 和 82 nM。Ro3280 还抑制其他几种癌细胞系，浓度较低[2]。
RO3280 对 5637 和 T24 人膀胱癌细胞具有细胞毒性，IC50 约为 100 nM。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ro3280 相关抗体:
体内研究
(In Vivo)

Ro3280 (RO3280，40 mg/kg，iv) 在植入 HT-29 结直肠癌细胞的小鼠异种移植模型中抑制 72% 的肿瘤生长，并且当更频繁地给药时，RO3280 完全抑制肿瘤生长[2]。
RO3280 (30 mg/kg，每 5 天一次，ip) 在裸鼠模型中显示出显著的抗膀胱癌活性[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

543.61

Formula

C27H35F2N7O3
CAS 号
性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
纯度 & 产品资料

纯度: 99.46%

COA (287 KB) HNMR (300 KB) RP-HPLC (249 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Ro3280 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ro32801062243-51-9Ro 3280Ro-3280Polo-like Kinase (PLK)Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-15161
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