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Background Information:
A highly potent, selective and ATP-competitive inhibitor of polo-like kinase 1 (Ki = 2.2 nM), and is 400-fold greater potency than PLK 2 and 3, currently in clinical trial.
Reference:
1. T.R. Rheault, et al., Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties. Bioorg. Med. Chem. Lett. 2010, 20(15), 4587-92.
2. K.A. Emmitte, et al., Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg. Med. Chem. Lett., 2009, 19(6), 1694-7.
APIM050169: GSK461364
CAS No.: 929095-18-1.
Molecular Formula: C27H28F3N5O2S ? 0.3HCl.
Molecular Weight: 554.5.
Purity: >99% by HPLC, 100% optical purity (Chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, and water with 2.0 eq. of HCl.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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