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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
PLK1
Available Sizes
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