PLK1-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PLK1-IN-4 

PLK1-IN-4 是一种有效且具有选择性的 PLK1 抑制剂，IC50 < 0.508 nM。PLK1-IN-4 对多种癌细胞具有广泛的抗增殖活性。PLK1-IN-4 诱导有丝分裂阻滞在 G2/M 期检查点，导致癌细胞凋亡 (apoptosis)。PLK1-IN-4 可用于肝细胞癌的研究。

PLK1-IN-4

PLK1-IN-4 Chemical Structure

CAS No. : 2622273-55-4

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生物活性

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma[1].

IC50 & Target

IC50:< 0.508 nM (PLK1) [1]
体外研究
(In Vitro)

PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells[1].
PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells[1].
PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest[1].
PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MDA-MB-231, HeLa, HCT 116, HT-29, HepG2, SMMC7721, A549 ,JeKo-1,K562, Karpas299, A375, DU-145 and L02[1]
Concentration: 0-5 μM
Incubation Time: 48 hours
Result: Exhibited excellent antiproliferative activities against HCC cells, with IC50s of 11.1 nM and 70.9 nM in HepG2 and SMMC7721 cells.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 10, 30, 60, 100 and 300 nM
Incubation Time: 0, 12, 24, 36 and 48 hours
Result: Induced apoptosis in cancer cells through G2/M arrest.

Western Blot Analysis

Cell Line: HepG2[1]
Concentration: 0, 10, 30, 60, 90 and 120 nM
Incubation Time: 24 hours
Result: Increased phosphorylation of PLK1, histone H3 and NPM and decreased phosphorylation of Cdc2 in a dose-dependent manner.

体内研究
(In Vivo)

PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhep of 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively[1].
PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner[1].
Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse[1].

IV (5 mg/kg)
C0 (ng/mL) 1790
T1/2 (h) 1.47
MRT0-inf (h) 0.808
MRT0-t (h) 0.704
AUC0-t (ng·h/mL) 767
AUC0-inf (ng·h/mL) 776
CL (mL/min/kg) 107
VdSS (L/kg) 107

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)[1]
Dosage: 30 mg/kg
Administration: Tail vein injection; once or twice daily, for 12 days
Result: Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model: ICR mouse[1]
Dosage: 5 mg/kg
Administration: IV; single (Pharmacokinetics Analysis)
Result: Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.

分子量

550.55

Formula

C24H25F3N6O4S
CAS 号

2622273-55-4
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.
参考文献

  • [1]. Deng Z, et al. Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma. Eur J Med Chem. 2020;206:112697.

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