GSK461364

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

Product Specifications

CAS Number

[929095-18-1]

Product Name Alternative

GSK461364A

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk461364.html

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic)

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

Molecular Formula

C27H28F3N5O2S

Molecular Weight

543.60

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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|[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.|[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.