PLK1-IN-4

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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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PLK1 PLK2 PLK3 PLK4

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC₅₀:< 0.508 nM (PLK1) ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	346.9 nM Compound: 31	Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
A549	IC₅₀	556.8 nM Compound: 31	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
DU-145	IC₅₀	200.9 nM Compound: 31	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HCT-116	IC₅₀	259.5 nM Compound: 31	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HeLa	IC₅₀	507.9 nM Compound: 31	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HepG2	IC₅₀	11.1 nM Compound: 31	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HT-29	IC₅₀	216 nM Compound: 31	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
JeKo-1	IC₅₀	70.4 nM Compound: 31	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
K562	IC₅₀	254.3 nM Compound: 31	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
KARPAS-299	IC₅₀	19.9 nM Compound: 31	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
L02	IC₅₀	91.8 nM Compound: 31	Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
MDA-MB-231	IC₅₀	953.5 nM Compound: 31	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
SMMC-7721	IC₅₀	70.9 nM Compound: 31	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]

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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