PLK1-IN-4

Cat. No.: HY-146792: FAQs
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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.

For research use only. We do not sell to patients.

PLK1-IN-4 Chemical Structure

CAS No. : 2622273-55-4

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC₅₀:< 0.508 nM (PLK1) ^[1]

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].

MedChemExpress (MCE) 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.

In Vivo

PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CL^hep 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
T_1/2 (h)	1.47
MRT_0-inf (h)	0.808
MRT_0-t (h)	0.704
AUC_0-t (ng·h/mL)	767
AUC_0-inf (ng·h/mL)	776
CL (mL/min/kg)	107
Vd_SS (L/kg)	107

MedChemExpress (MCE) 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 (T_1/2) of 1.47 h, moderate exposure with an area under the curve (AUC_0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vd_ss) of 5.21 L/kg.

Molecular Weight

550.55

Formula

C₂₄H₂₅F₃N₆O₄S

CAS No.

2622273-55-4

SMILES

COC1=C(C=C2C(CCN2C(CN(C)C)=O)=C1)NC3=NC=C(C(NC4=C(SC=C4)C(OC)=O)=N3)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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 carcino [Content Brief]

PLK1-IN-4 Related Classifications

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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-42622273-55-4Polo-like Kinase (PLK)Hepatocellular carcinomaAnticancerSelectiveHepG2Inhibitorinhibitorinhibit

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