GSK-461364
GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.
1: Liu-Sullivan N, Zhang J, Bakleh A, Marchica J, Li J, Siolas D, Laquerre S, Degenhardt YY, Wooster R, Chang K, Hannon GF, Powers S. Pooled shRNA screen for sensitizers to inhibition of the mitotic regulator polo-like kinase (PLK1). Oncotarget. 2011 Dec;2(12):1254-64. PubMed PMID: 22248814.
2: Olmos D, Barker D, Sharma R, Brunetto AT, Yap TA, Taegtmeyer AB, Barriuso J, Medani H, Degenhardt YY, Allred AJ, Smith DA, Murray SC, Lampkin TA, Dar MM, Wilson R, de Bono JS, Blagden SP. 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. Epub 2011 Apr 1. PubMed PMID: 21459796.
3: Schöffski P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70. Epub 2009 May 27. Review. PubMed PMID: 19474163.
2: Olmos D, Barker D, Sharma R, Brunetto AT, Yap TA, Taegtmeyer AB, Barriuso J, Medani H, Degenhardt YY, Allred AJ, Smith DA, Murray SC, Lampkin TA, Dar MM, Wilson R, de Bono JS, Blagden SP. 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. Epub 2011 Apr 1. PubMed PMID: 21459796.
3: Schöffski P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70. Epub 2009 May 27. Review. PubMed PMID: 19474163.
| Chemical | |
|---|---|
| CAS Num | 929095-18-1 |
| Chemical Formula | C27H28F3N5O2S |
| Molecular Weight | 543.60373 |
| IUPAC Chemical Name | (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide |
| Exact Mass | 543.19158 |
| Elemental Analysis | C, 59.66; H, 5.19; F, 10.48; N, 12.88; O, 5.89; S, 5.90 |
| Synonym | GSK461364; GSK 461364; GSK-461364; GSK461364A; GSK 461364A; GSK-461364A. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C1=C(O[C@@H](C2=CC=CC=C2C(F)(F)F)C)C=C(N3C=NC4=CC=C(CN5CCN(C)CC5)C=C34)S1)N |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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