533380 Sigma-AldrichPolo-like Kinase Inhibitor VI, NMS-P937 - CAS 1034616-18-6 - Calbiochem
Polo-Like Kinase Inhibitor VI, NMS-P937, CAS 1034616-18-6, is a cell-permeable, highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM).
More>> Polo-Like Kinase Inhibitor VI, NMS-P937, CAS 1034616-18-6, is a cell-permeable, highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM). Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: PLK1 Inhibitor II, NMS P937, NMS-1286937
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Overview
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Key Specifications Table
Empirical Formula | CAS # |
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C₂₄H₂₇F₃N₈O₃ | 1034616-18-6 |
Pricing & Availability
Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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5.33380.0001 |
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Glass bottle | 5 mg |
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Description | |
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Overview | A cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC50 > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC50 = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC50 = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC50 = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water. |
Catalogue Number | 533380 |
Brand Family | Calbiochem® |
Synonyms | PLK1 Inhibitor II, NMS P937, NMS-1286937 |
References | |
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References | Casolaro, A., et al. 2013. PLoS One 8, e58424. Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006. Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969. |
Product Information | |
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CAS number | 1034616-18-6 |
Form | Pale yellow solid |
Hill Formula | C₂₄H₂₇F₃N₈O₃ |
Chemical formula | C₂₄H₂₇F₃N₈O₃ |
Reversible | Y |
Quality Level | MQ100 |
Applications |
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Biological Information | |
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Primary Target | Plk1 |
Primary Target IC<sub>50</sub> | 2 nM |
Purity | ≥98% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
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Materials Information |
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Safety Information according to GHS |
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Product Usage Statements |
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Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Documentation
References
Reference overview |
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Casolaro, A., et al. 2013. PLoS One 8, e58424. Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006. Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969. |
Data Sheet | ||||||||||||||||||||||||||||
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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