GSK461364
Cat. No.:YN290487
CAS No. :929095-18-1
产品名称: | GSK461364 |
CAS No.: | 929095-18-1 |
Chemical Name: | 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide |
Synonyms: | GSK461364A |
分子量: | 543.60 |
分子式: | C₂₇H₂₈F₃N₅O₂S |
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 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | GSK461364 是选择性,可逆,ATP竞争性的PLK1抑制剂,Ki值为 2.2 nM。 |
IC50和靶点: | [{name:"PLK1:2.2 nM (Ki)"}] |
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Clinical Trial: | |
Solvent & Solubility: |
Schöffski, P.Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncologyOncologist14(6),559-570(2009)
Gilmartin, A.G., Bleam, M.R., Richter, M.C., et al.Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosisCancer Res.69(17),6969-6977(2009)
Degenhardt, Y., Greshock, J., Laquerre, S., et al.Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instabilityMol. Cancer Ther.9(7),2079-2089(2010)
Danovi, D., Folarin, A., Gogolok, S., et al.A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1PLoS One8(10),1-13(2013)