GSK461364 (Synonyms: GSK461364A)

Name: GSK461364
Brand: MedChemExpress
SKU: HY-50877
Rating: 5.0 (20 reviews)

Cat. No.: HY-50877 Purity: 98.68%: Data Sheet
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GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a K_i value of 2.2 nM.

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

CAS No. : 929095-18-1

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 20 publication(s) in Google Scholar

20 Publications Citing Use of MCE GSK461364

Cell Proliferation/Viability Assay

Flow Cytometry

Cell Imaging/Staining

In Vivo Efficacy Study

ELISA

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; Western blot analysis of PLK1 protein levels from GSK461364A (GSK) treated U251 cells; actin levels are measured as a loading control.

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; U251 cells were exposed to GSK461364A (GSK) or DMSO control for two hours. Colony-forming efficiency was determined 10–14 days later and % survival generated after normalizing to DMSO control. The results showed that the inhibitory effect of GSK461364A on colony formation was dose-dependent, with a concentration of 1 nM achieving a 50% inhibition rate.

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; To assess cell cycle phase distribution GBM U251 cells were exposed to GSK461364A (GSK) or DMSO control for two hours and then stained with propidium iodide 24 hours later for flow cytometry analysis.

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; To assess mitotic catastrophe represented as the number of cells with multilobulated giant nuclei (left two panels) and cells with abnormal mitoses (right panel) (white arrows), U251 cells stained with anti-tubulin antibody (red) and nuclei were visualized with DAPI (blue) staining and nuclear fragmentation was evaluated in 150 cells per treatment per experiment and plotted against the drug concentration and time intervals. The results showed that the number of cells undergoing mitotic catastrophe significantly increased at the 48- and 72-hour time points in cells treated with GSK461364A (GSK) (10 nM).

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; U251 cells were implanted subcutaneously into nude mice and tumor growth was monitored over time. Tumors grown to ≈172 mm³ were randomized to one of four treatment arms: vehicle treated control, GSK461364A (25 mg/kg), GSK461364A (50 mg/kg), or GSK461364A (100 mg/kg). Mice were treated with two doses of GSK461364A or DMSO control four days apart. Tumor volume plotted as the mean volume ± SD.

: GSK461364 purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2013 Sep;49(14):3020-8. [Abstract]; U251 cells were exposed to GSK461364A (GSK, 1-10 nM) or DMSO control for 2 hours before irradiation. H2AX levels measured at 24 hours and optical density at 450 nm was plotted.

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Description

GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a K_i value of 2.2 nM.

IC₅₀ & Target^[3]

PLK1

2.2 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
A-427	GI₅₀	22.8 nM Compound: GSK461364A	Antiproliferative activity against human A-427 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A-427 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A-431	GI₅₀	16.65 nM Compound: GSK461364A	Antiproliferative activity against human A-431 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A-431 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A2780	GI₅₀	28.1 nM Compound: GSK461364A	Antiproliferative activity against human A2780 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A2780 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A375P	GI₅₀	23.65 nM Compound: GSK461364A	Antiproliferative activity against human A375P cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A375P cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A498	GI₅₀	40.35 nM Compound: GSK461364A	Antiproliferative activity against human A498 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A498 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A549	GI₅₀	33.95 nM Compound: GSK461364A	Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
A704	GI₅₀	183.05 nM Compound: GSK461364A	Antiproliferative activity against human A704 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A704 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
ASPC1	GI₅₀	22.3 nM Compound: GSK461364A	Antiproliferative activity against human ASPC1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human ASPC1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
BT-474	GI₅₀	7091.05 nM Compound: GSK461364A	Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
BT-549	GI₅₀	23.05 nM Compound: GSK461364A	Antiproliferative activity against human BT-549 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BT-549 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
BXPC-3	GI₅₀	23.1 nM Compound: GSK461364A	Antiproliferative activity against human BXPC-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human BXPC-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
COLO 205	GI₅₀	14.2 nM Compound: GSK461364A	Antiproliferative activity against human COLO 205 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human COLO 205 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
Calu-1	GI₅₀	186 nM Compound: GSK461364A	Antiproliferative activity against human Calu-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Calu-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
Calu-3	GI₅₀	35.65 nM Compound: GSK461364A	Antiproliferative activity against human Calu-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Calu-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
DLD-1	GI₅₀	48.85 nM Compound: GSK461364A	Antiproliferative activity against human DLD-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human DLD-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
DU-145	GI₅₀	24.2 nM Compound: GSK461364A	Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
H322	GI₅₀	20.25 nM Compound: GSK461364A	Antiproliferative activity against human H322 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human H322 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HCC1937	GI₅₀	4794.9 nM Compound: GSK461364A	Antiproliferative activity against human HCC1937 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC1937 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HCC1954	GI₅₀	14.05 nM Compound: GSK461364A	Antiproliferative activity against human HCC1954 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCC1954 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HCT-116	GI₅₀	50.45 nM Compound: GSK461364A	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HCT-15	GI₅₀	90.85 nM Compound: GSK461364A	Antiproliferative activity against human HCT-15 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HCT-15 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HEK-293T	IC₅₀	1 nM Compound: 1; GSK-461364	Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
HL-60	GI₅₀	17.5 nM Compound: GSK461364A	Antiproliferative activity against human HL-60 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HN5	GI₅₀	15.45 nM Compound: GSK461364A	Antiproliferative activity against human HN5 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HN5 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HT-1080	GI₅₀	24.55 nM Compound: GSK461364A	Antiproliferative activity against human HT-1080 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HT-1080 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HT-29	GI₅₀	8.1 nM Compound: GSK461364A	Antiproliferative activity against human HT-29 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HT-29 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HUVEC	IC₅₀	7 nM Compound: GSK461364A	Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
HeLa	GI₅₀	21.8 nM Compound: GSK461364A	Antiproliferative activity against human HeLa cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human HeLa cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
Hep 3B2	GI₅₀	35.75 nM Compound: GSK461364A	Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
Jurkat	GI₅₀	18.6 nM Compound: GSK461364A	Antiproliferative activity against human Jurkat cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Jurkat cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
K562	GI₅₀	19.45 nM Compound: GSK461364A	Antiproliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human K562 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
LNCaP	GI₅₀	15.35 nM Compound: GSK461364A	Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
LoVo	GI₅₀	12.2 nM Compound: GSK461364A	Antiproliferative activity against human LoVo cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human LoVo cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MCF7	GI₅₀	6.4 nM Compound: GSK461364A	Antiproliferative activity against human MCF7 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MDA-MB-231	GI₅₀	9.15 nM Compound: GSK461364A	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MDA-MB-231	IC₅₀	1 nM Compound: 1; GSK-461364	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MDA-MB-453	GI₅₀	13.45 nM Compound: GSK461364A	Antiproliferative activity against human MDA-MB-453 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-453 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MDA-MB-468	GI₅₀	6.35 nM Compound: GSK461364A	Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MIA PaCa-2	GI₅₀	39.9 nM Compound: GSK461364A	Antiproliferative activity against human MIA PaCa-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MIA PaCa-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
MM1.S	IC₅₀	1 nM Compound: 1; GSK-461364	Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MV4-11	GI₅₀	0.679 μM Compound: GSK-461364	Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay	[PMID: 26191363]
MX1	GI₅₀	12.1 nM Compound: GSK461364A	Antiproliferative activity against human MX1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human MX1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H1155	GI₅₀	14.45 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H1155 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1155 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H1299	GI₅₀	61.4 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H1299 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1299 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H157	GI₅₀	25.25 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H157 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H157 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H358	GI₅₀	13.4 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H358 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H358 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H460	GI₅₀	37.8 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H460 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H460 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H522	GI₅₀	16.9 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H522 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H522 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H727	GI₅₀	45.25 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H727 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H727 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-H82	GI₅₀	4.85 nM Compound: GSK461364A	Antiproliferative activity against human NCI-H82 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H82 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
NCI-N87	GI₅₀	21.5 nM Compound: GSK461364A	Antiproliferative activity against human NCI-N87 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-N87 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
OVCAR-3	GI₅₀	12.95 nM Compound: GSK461364A	Antiproliferative activity against human OVCAR-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OVCAR-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
OVCAR-4	GI₅₀	24.25 nM Compound: GSK461364A	Antiproliferative activity against human OVCAR-4 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OVCAR-4 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
OVCAR-8	GI₅₀	20.45 nM Compound: GSK461364A	Antiproliferative activity against human OVCAR-8 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human OVCAR-8 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
PANC-08-13	GI₅₀	18.9 nM Compound: GSK461364A	Antiproliferative activity against human PANC-08-13 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human PANC-08-13 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
PANC-1	GI₅₀	44.85 nM Compound: GSK461364A	Antiproliferative activity against human PANC-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human PANC-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
PC-3	GI₅₀	14663 nM Compound: GSK461364A	Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
RKO	GI₅₀	62.9 nM Compound: GSK461364A	Antiproliferative activity against human RKO cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human RKO cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
RPMI-8226	GI₅₀	22.5 nM Compound: GSK461364A	Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
Raji	GI₅₀	25.3 nM Compound: GSK461364A	Antiproliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human Raji cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SAOS-2	GI₅₀	14.15 nM Compound: GSK461364A	Antiproliferative activity against human SAOS-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SAOS-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SCLC	GI₅₀	17.4 nM Compound: GSK461364A	Antiproliferative activity against human SCLC cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SCLC cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SJSA-1	GI₅₀	24.4 nM Compound: GSK461364A	Antiproliferative activity against human SJSA-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SJSA-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-BR-3	GI₅₀	15.75 nM Compound: GSK461364A	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-MEL-2	GI₅₀	14 nM Compound: GSK461364A	Antiproliferative activity against human SK-MEL-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-2 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-MEL-28	GI₅₀	380.7 nM Compound: GSK461364A	Antiproliferative activity against human SK-MEL-28 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-28 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-MEL-5	GI₅₀	28.35 nM Compound: GSK461364A	Antiproliferative activity against human SK-MEL-5 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL-5 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-MEL3	GI₅₀	17.6 nM Compound: GSK461364A	Antiproliferative activity against human SK-MEL3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-MEL3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SK-OV-3	GI₅₀	28.9 nM Compound: GSK461364A	Antiproliferative activity against human SK-OV-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SK-OV-3 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SW-620	GI₅₀	6.6 nM Compound: GSK461364A	Antiproliferative activity against human SW620 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW620 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
SW480	GI₅₀	129.5 nM Compound: GSK461364A	Antiproliferative activity against human SW480 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human SW480 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
T-24	GI₅₀	42.3 nM Compound: GSK461364A	Antiproliferative activity against human T24 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human T24 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
T47D	GI₅₀	9162.07 nM Compound: GSK461364A	Antiproliferative activity against human T47D cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human T47D cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
THP-1	GI₅₀	11.85 nM Compound: GSK461364A	Antiproliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human THP-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
U-87MG ATCC	GI₅₀	7.45 nM Compound: GSK461364A	Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
U2OS	GI₅₀	41.7 nM Compound: GSK461364A	Antiproliferative activity against human U2OS cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human U2OS cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]
ZR-75-1	GI₅₀	46.45 nM Compound: GSK461364A	Antiproliferative activity against human ZR-75-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human ZR-75-1 cells assessed as growth inhibition incubated for 72 hrs by celltiter-glo assay	[PMID: 19690138]

In Vitro

GSK461364 is a potent, selective, and reversible ATP-competitive Plk1 inhibitor (K_i, 2.2 nM) with at least 390-fold greater selectivity for Plk1 than for Plk2 and Plk3 and 1,000-fold greater selectivity than for a panel of 48 other kinases^[1]. GSK461364 (GSK461364A, 250 nM) inhibiting plk1 causes prolonged mitotic delay, aberrant mitotic exit, and p53 activation in A549 and PL45 cells. Knockdown of p53 significantly enhances the sensitivity of the cells to GSK461364A (30 or 300 nM) in preventing outgrowth in A549 and NCI-H460 cells, compared with cells with nonsilencing control siRNA^[2]. GSK461364 can inhibits cell growth of most proliferating cancer cell lines, and suppresses 89% of cancer cell line (66 of 74 lines) proliferation, with a GI₅₀ (concentration required to inhibit 50% cell growth) of ≤100 nM. GSK461364 (GSK461364A, >20 nM) blocks cells in G2-M phase with reduction of cells in G1 phase of A549 lung carcinoma line. GSK461364 (10-250 nM) blocks cells in G2 and M phases of the cell cycle and causes M-phase caspase-3/caspase-7 activation in cancer cells^[3]. GSK461364 (0.5-2 μM) decreases level of PLK1 and pCDC25C, and cuases a dose- and time-dependent increase in pHisH3, an indicator of mitotic arrest in OS cell lines^[4].

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

In Vivo

GSK461364 (50 mg/kg) exhibits various degrees of tumor growth delay (TGD) in multiple xenograft tumor models by i.p. one dose every 2 days repeated twelve times (q2d×12)^[1].

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

Clinical Trial

Molecular Weight

543.60

Formula

C₂₇H₂₈F₃N₅O₂S

CAS No.

929095-18-1

Appearance

Solid

Color

Off-white to gray

SMILES

O=C(C(SC(N1C=NC2=CC=C(C=C12)CN3CCN(CC3)C)=C4)=C4O[C@@H](C5=CC=CC=C5C(F)(F)F)C)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (91.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8396 mL	9.1979 mL	18.3959 mL
5 mM	0.3679 mL	1.8396 mL	3.6792 mL
10 mM	0.1840 mL	0.9198 mL	1.8396 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (253 KB) HNMR (181 KB) LCMS (503 KB)

Handling Instructions (2659 KB)

References

[1]. Olmos D, et al. Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 inhibitor, in patients with advanced solid malignancies. Clin Cancer Res. 2011 May 15;17(10):3420-30. [Content Brief]

[2]. Degenhardt Y, et al. Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability. Mol Cancer Ther. 2010 Jul;9(7):2079-89 [Content Brief]

[3]. Gilmartin AG, et al. Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis. Cancer Res. 2009 Sep 1;69(17):6969-77. [Content Brief]

[4]. Chou YS, et al. Cytotoxic mechanism of PLK1 inhibitor GSK461364 against osteosarcoma: Mitotic arrest, apoptosis, cellular senescence, and synergistic effect with paclitaxel. Int J Oncol. 2016 Mar;48(3):1187-94. [Content Brief]

Kinase Assay ^[3]	Kinase reactions are performed in a final assay volume of 10 μL using the Z'-Lyte Assay kit (Ser/Thr peptide 16). Briefly, reactions contained 50 mM HEPES (pH 7.5), 10 mM MgCl₂, 1 mM EGTA, 1 mM DTT, 0.01% Brij 35, 0.01 mg/mL casein, 200 μM ATP, 200 μM Polo Box peptide (NH2-MAGPMQS[pT]PLNGAKK-OH), and 6 nM recombinant Plk1 (H6-tev-PLK 1-603). Plk1 is preincubated for 60 min in the presence or absence of 0 to 1,000 nM GSK461364. Reactions are then initiated by the addition of 2 μM peptide. After 15 min at 23°C, reactions are quenched and processed according the Z'-Lyte protocol and read on an plate reader. Raw fluorescence values are converted to concentration of product formed using substrate and product standards. IC₅₀ values are determined using a two-parameter fit (Hill coefficient and IC₅₀) using GraFit software. Because the potency of inhibition for GSK461364 is observed to vary as a function of the ATP concentration in a manner consistent with an ATP-competitive mode of inhibition, an upper limit for the K_i^app for GSK461364 is determined by applying the Cheng-Prusoff relationship for a competitive inhibitor (ATP K_m^app=16 μM) to the IC₅₀ value obtained with 60 min preincubation of GSK461364. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	Cell lines grow in the recommended media at 37°C, 5% CO₂ in a humidified incubator. Cells are plated in triplicate 96-well microtiter plates at 1,000 cells per well in culture media. GSK461364 (GSK461364A) dissolved in DMSO or negative control (0.1% DMSO) are added the following day, and one plate is harvested with 50 μL of CellTiter-Glo for a time 0 (T=0) measurement. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Cells are implanted in Nude mice and grown as tumor xenografts. Dosing began when tumors achieve appr 100 mm³. GSK461364 (GSK461364A) or the vehicle [4% DMA/Cremaphore (50:50), pH 5.6] is given i.p. to mice every 2 d (q2d×6, q2d×12) or every 4 d (q4d×3) at nominal dose levels of 25, 50, and 100 mg/kg/dose. Results are reported as median tumor volume for n=7 to 8 mice. Paclitaxel (30 mg/kg i.v.; q4d×3) is used as a positive control for comparison. Tumors are measured thrice a week with Vernier calipers, and tumor volume is calculated from two-dimensional measurements using an equation approximating the volume of a prolate ellipsoid [tumor volume mm³=(length × width²) × 0.5]. The maximum tolerated dose is defined as the highest dose that produces >20% mortality or >20% weight loss (appr 4 g). Antitumor activity is defined as tumor growth delay (TGD), partial regression (PR), or complete regression (CR). TGD represents the time differential between the treated and control tumors to reach a predetermined tumor volume of 1,000 mm³. PR is defined as a decrease in an individual tumor volume to one-half the initial starting volume for at least 1 wk (three consecutive measurements). CR is defined as a decrease in an individual tumor volume to <13 mm³ for at least 1 wk. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Olmos D, et al. Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 inhibitor, in patients with advanced solid malignancies. Clin Cancer Res. 2011 May 15;17(10):3420-30. [Content Brief] [2]. Degenhardt Y, et al. Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability. Mol Cancer Ther. 2010 Jul;9(7):2079-89 [Content Brief] [3]. Gilmartin AG, et al. Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis. Cancer Res. 2009 Sep 1;69(17):6969-77. [Content Brief] [4]. Chou YS, et al. Cytotoxic mechanism of PLK1 inhibitor GSK461364 against osteosarcoma: Mitotic arrest, apoptosis, cellular senescence, and synergistic effect with paclitaxel. Int J Oncol. 2016 Mar;48(3):1187-94. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8396 mL	9.1979 mL	18.3959 mL	45.9897 mL
	5 mM	0.3679 mL	1.8396 mL	3.6792 mL	9.1979 mL
	10 mM	0.1840 mL	0.9198 mL	1.8396 mL	4.5990 mL
	15 mM	0.1226 mL	0.6132 mL	1.2264 mL	3.0660 mL
	20 mM	0.0920 mL	0.4599 mL	0.9198 mL	2.2995 mL
	25 mM	0.0736 mL	0.3679 mL	0.7358 mL	1.8396 mL
	30 mM	0.0613 mL	0.3066 mL	0.6132 mL	1.5330 mL
	40 mM	0.0460 mL	0.2299 mL	0.4599 mL	1.1497 mL
	50 mM	0.0368 mL	0.1840 mL	0.3679 mL	0.9198 mL
	60 mM	0.0307 mL	0.1533 mL	0.3066 mL	0.7665 mL
	80 mM	0.0230 mL	0.1150 mL	0.2299 mL	0.5749 mL

GSK461364 Related Classifications

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:

GSK461364929095-18-1GSK461364AGSK 461364GSK-461364Polo-like Kinase (PLK)Inhibitorinhibitorinhibit

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GSK461364 (Synonyms: GSK461364A)

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