2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-12

PLK1-IN-12 是一种高选择性、具有口服活性的 PLK1 抑制剂，IC50 为 20 nM。PLK1-IN-12 对 PLK1 的选择性高于 PLK2 (IC50: >10000 nM) 和 PLK3 (IC50: 3953 nM)。PLK1-IN-12 在广泛的细胞系中表现出抗癌效力。PLK1-IN-12 能够用于抗白血病研究。

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PLK1-IN-12 Chemical Structure

PLK1-IN-12 Chemical Structure

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Customer Review

PLK1-IN-12 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

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research[1].

IC50 & Target[1]

PLK1

20 nM (IC50)

PLK2

>10000 nM (IC50)

PLK3

3953 nM (IC50)

体外研究
(In Vitro)

PLK1-IN-12 (Compound B31) (0.508 nM-10 μM，24 小时) 在 H460 (IC50: 12 nM)、A549 (IC50: 32 nM)、SW620 (IC50: 8.2 nM)、HL-60 (IC50: 59 nM)、K562 (IC50: 0.08 nM) 和 CCRF-CEM (IC50: 41 nM) 细胞系中均表现抗增殖作用[1]。
PLK1-IN-12 (1 μM，5 分钟) 在人、小鼠和犬肝微粒体中均表现较快的清除率 (Clint: 68.3-210 μL/min/mg protein)[1]。
PLK1-IN-12 (0.1-30 μM，24 小时) 对 HEK293T 细胞具有较低的细胞活力抑制效果 (68%)[1]。
PLK1-IN-12 (0.4-100 μM) 对 hERG 钾通道的抑制作用低 (IC50: 44.2 μM)，表明心脏毒性风险低[1]。
PLK1-IN-12 (10 μM， 5-30 分钟) 对 CYP1A2、CYP3A4、CYP2D6、CYP2B6 和 CYP2C8 无抑制，对 CYP2C9 和 CYP2C19 仅有微弱的抑制作用。表明在人和大鼠肝细胞中均稳定，发生药物相互作用的可能性较低[1]。

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

PLK1-IN-12 相关抗体:

Cell Proliferation Assay[1]

Cell Line: H460、PC-9、A549、SW620、HL-60、K562、CCRF-CEM and KG-1 cell lines
Concentration: 1.00 × 10-5, 3.33 × 10-6, 1.11 × 10-6, 3.7 × 10-7, 1.23 × 10-7, 4.12 × 10-8, 1.37 × 10-8, 4.57 × 10-9, 1.52 × 10-9, and 5.08 × 10-10 mol/L
Incubation Time: 24 h
Result: Showed antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines.

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 0.1, 0.3, 1, 3, 10, and 30 μM
Incubation Time: 24 h
Result: Had a low inhibitory effect on cell viability of HEK293T cells (68%).
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. Cmax 264 ng/mL
Mice 10 mg/kg p.o. Cmax 328 ng/mL
Mice 1 mg/kg i.v. Tmax 0.083 hr
Mice 10 mg/kg p.o. Tmax 0.75 hr
Mice 1 mg/kg i.v. T1/2 0.59 hr
Mice 10 mg/kg p.o. T1/2 1.2 hr
Mice 1 mg/kg i.v. AUC0-t 181 ng·h/mL
Mice 10 mg/kg p.o. AUC0-t 820 ng·h/mL
Mice 1 mg/kg i.v. AUC0-inf 183 ng·h/mL
Mice 10 mg/kg p.o. AUC0-inf 825 ng·h/mL
Mice 1 mg/kg i.v. CL 91 mL/min/kg
Mice 10 mg/kg p.o. MRT0-t 2.0 hr
Mice 1 mg/kg i.v. MRT0-t 0.66 hr
Mice 10 mg/kg p.o. F 45 %
Mice 1 mg/kg i.v. Vss 0.0036 L/kg
体内研究
(In Vivo)

PLK1-IN-12 (Compound B31) (10/20 mg/kg，灌胃，每周 2 次，11 天) 可抑制小鼠皮下 K562 细胞移植肿瘤模型中肿瘤的生长[1]。
PLK1-IN-12 (500 mg/kg，灌胃，每天 1 次，7 天) 对小鼠各个器官没有组织损伤或毒性[1]。

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

Animal Model: Subcutaneous K562 cell transplantation tumor model, Male BALB/c mice (6–8 weeks old, weighing 18–20 g)[1]
Dosage: 10/20 mg/kg
Administration: Intragastric (i.g.), twice weekly for 11 d
Result: Inhibited tumor growth.
Animal Model: Acute toxicity test[1]
Dosage: 500 mg/kg
Administration: Intragastric (i.g.), once daily for 7 d
Result: Compared with the mice in the positive control group, there was no significant change in body weight, and no obvious damage to the heart, kidney, lung, liver and spleen.
分子量

558.12

Formula

C28H40ClN7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PLK1-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

PLK1-IN-12Polo-like Kinase (PLK)Anti-cancerH460 cell linesA549 cell linesSW620 cell linesHL-60 cell linesK562 cell linesCCRF-CEM cell linessubcutaneous K562 cell transplantation tumor modelAnti-leukemiaInhibitorinhibitorinhibit

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