2. Cell Cycle/DNA Damage Apoptosis
  3. Polo-like Kinase (PLK) c-Myc Apoptosis
  4. PLK1-IN-13

PLK1-IN-13 是一种选择性和口服活性的 PLK1 抑制剂 (IC50: 0.27 nM)。PLK1-IN-13 还抑制 PLK2 (IC50: 12.72 nM) 和 PLK3 (IC50: 4.12 nM)。PLK1-IN-13将细胞停滞在 G2 期，诱导细胞凋亡 (apoptosis) 并下调增殖相关致癌基因 c-MYC 的转录。PLK1-IN-13 抑制肿瘤生长，可用于急性髓系白血病 (AML) 的研究。

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PLK1-IN-13 Chemical Structure

PLK1-IN-13 Chemical Structure

CAS No. : 3038489-48-1

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PLK1-IN-13 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-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

PLK1

0.27 nM (IC50)

PLK2

12.72 nM (IC50)

PLK3

4.12 nM (IC50)

体外研究
(In Vitro)

PLK1-IN-13 (72 h) (Compound WD6) 对 MDA-MB-231 (IC50: 9.5 nM) 和 MV4-11 细胞 (IC50: 23.3 nM) 有抗增殖活性，对 MCF-7 和 HCT-116 的 IC50 分别为 47.1 nM 和 59.9 nM[1]。
PLK1-IN-13 对 CYP2C9 (IC50: 7.39 μM)、CYP2C19 (IC50: 14 μM), CYP2D6 (IC50: 13.8 μM) 和 CYP3A4 (IC50: 17.3 μM) 有较弱的抑制作用，表明 PLK1-IN-13 可能具有较低的药物相互作用[1]。
PLK1-IN-13 (2.92 nM-46.6 nM，72 小时) 诱导 MV4-11 细胞 G2/M 细胞周期停滞并诱导凋亡[1]。
PLK1-IN-13 (0-1 μM，24 小时) 下调 MV4-11 细胞中增殖相关致癌基因 c-MYC 的转录[1]。

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

PLK1-IN-13 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 2.92 nM, 5.83 nM, 11.6 nM, 23.3 nM, and 46.6 nM
Incubation Time: 72 h
Result: Increased the cell apoptosis rate, ranging from 3.29% to 67.7% in a concentration-dependent manner.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 5.82 hr
Rat 10 mg/kg i.g. T1/2 7.59 hr
Rat 1 mg/kg i.v. AUC0-t 8.35 μg·h/mL
Rat 10 mg/kg i.g. Tmax 5.53 hr
Rat 10 mg/kg i.g. Cmax 1900 ng/mL
Rat 10 mg/kg i.g. AUC0-t 29.3 μg·h/mL
体内研究
(In Vivo)

PLK1-IN-13 (Compound WD6) (20 mg/kg，口服，每天一次，连续 19 天) 可抑制 MV4-11 异种移植小鼠模型中的肿瘤生长 (TGI = 91.2 %)[1]。
PLK1-IN-13 (10、20 mg/kg，口服) 在 SD 大鼠中表现出良好的半衰期、高血浆暴露量和中等生物利用度[1]。

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

Animal Model: subcutaneous xenograft mouse models of MV4-11, Balb/c nude mice [1]
Dosage: 20 mg/kg
Administration: p.o., once a day for 19 consecutive days.
Result: Inhibited the tumor growth (TGI=91.2%).
Showed no significant weight loss or death in mice.
分子量

577.74

Formula

C29H39N9O2S
CAS 号
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-13 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 *
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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)
× = ×
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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:

PLK1-IN-133038489-48-1Polo-like Kinase (PLK)c-MycApoptosisMycAcute myeloid leukemiaAMLMV4-11cell-cycle arrestc-mycInhibitorinhibitorinhibit

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