1. Cell Cycle/DNA Damage Epigenetics
  2. Polo-like Kinase (PLK) Epigenetic Reader Domain
  3. PLK1-IN-6

PLK1-IN-6 是一种有效和选择性的 PLK1 抑制剂,IC50 值为 0.45 nM。PLK1-IN-6 对癌细胞显示出显着的抗增殖活性。

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PLK1-IN-6

PLK1-IN-6 Chemical Structure

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     可免费申领三个不同产品的试用装。

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Customer Review

查看 Polo-like Kinase (PLK) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells[1].

IC50 & Target[1]

PLK1

0.45 nM (IC50)

PLK2

5.73 nM (IC50)

PLK3

7.56 nM (IC50)

BRD4

156.3 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
26 nM
Compound: 21g
Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
[PMID: 36889251]
MCF7 IC50
8.64 nM
Compound: 21g
Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
[PMID: 36889251]
MDA-MB-231 IC50
14.8 nM
Compound: 21g
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
[PMID: 36889251]
MV4-11 IC50
47.4 nM
Compound: 21g
Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
[PMID: 36889251]
体外研究
(In Vitro)

PLK1-IN-6 (compound 21 g) 对四种肿瘤来源的细胞系显示出显着的抗增殖活性 (MCF-7 IC50=8.64 nM, HCT-116 IC50=26.0 nM, MDA-MB-231 IC50=14.8 nM and MV4-11 IC50=47.4 nM)[1] .
PLK1-IN-6 代谢适中,在人肝微粒体中的半衰期为 25.7 min[1]

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

体内研究
(In Vivo)

PLK1-IN-6 (compound 21 g) (1 mg/kg; i.v.) 在 Sprague Dawley 大鼠中表现出良好的半衰期 (10.1 h) 和血浆浓度曲线下面积[1]。< br/> PLK1-IN-6 (10 mg/kg; i.g.) 在 Sprague Dawley 大鼠中表现出低清除率值和高血浆暴露量 (26800 ng•h/mL),具有良好的生物利用度 (11.4%)[1]
PLK1-IN-6 (10 mg/kg; i.g.) 在 Balb/c 小鼠中表现出长半衰期 (2.73 h),高血浆暴露 (11227 ng•h/mL) 和出色的生物利用度 (77.4%)
[ 1]
PLK1-IN-6 (20 mg/kg; i.g.) 对小鼠没有明显的毒性[1]

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

分子量

547.65

Formula

C28H37N9O3

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
  • 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.

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产品名称:
PLK1-IN-6
目录号:
HY-149100
需求量: