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Poloppin

Catalog No.GC60294

Poloppin es un potente inhibidor de penetraciÓn celular de la cinasa tipo Polo mitÓtica (PLK) (IC50 = 26,9 μM) y previene la interacciÓn proteÍna-proteÍna a través del dominio Polo-box (PBD) (Kd = 29,5 μM). Poloppin elimina selectivamente las células que expresan KRAS mutante, aumentando la muerte en la mitosis. Poloppin se utiliza para el estudio de cÁnceres con mutaciÓn KRAS como agente Único o en combinaciÓn con inhibidores de c-MET.

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Poloppin Chemical Structure

Cas No.: 683808-78-8

Tamaño Precio Disponibilidad Cantidad
5mg
260,00 $
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10mg
445,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors[1].

Poloppin (0-200 μM) competitively inhibits the binding of a TAMRA-labeled substrate peptide to the PLK1 PBD, exhibiting an IC50 value of 26.9 μM in an FP assay; the isothermal titration calorimetry of Poloppin binding to the PBD domain of PLK1 with a Kd of 29.5 μM[1].Poloppin (0-100 μM) triggers a dose-dependent mitotic arrest and induces multiple anomalies in mitosis in cells, the EC50 value is 29.9 μM. In representative images of U2OS cells with 12.5 μM Poloppin, <5% of cells exhibit normal metaphase chromosome alignment, and shows bipolar or disordered spindles and non-congressed chromosomes in cells[1].Poloppin (0-200 μM; 24 hours) inhibits SW48 isogenic parental or KRAS G12D cells growth with GI50 values of 13.7 μM and 5.3 μM, respectively. It inhibits KRAS wild-type p53 and KRAS MUT p53 MEFs cells with GI50 values of 51.1 and 49.5 μM, respectively. When the medium is added 500nM 4-OH Tamoxifen to the culture media overnight, Poloppin inhibits KRAS wild-type p53 and KRAS MUT p53 MEFs cells with GI50 values of 43.7 μM and 17.6 μM, respectively[1].Poloppin (0-10 μM; 72 hours) sensitizes mutant KRAS-expressing cells to inhibitors of the c-MET tyrosine kinase. SW48 cell bearing mutant KRAS are sensitized to Poloppin after inhibition of c-MET, the GI50 values of Poloppin combination with Crizotinb are 0.23 uM and 0.08 uM, respectively in SW48 KRAS WT and KRAS G12D cells. In the contrast, the GI50 values are 0.56 uM and 0.63 uM in SW48 KRAS WT or KRAS MUT cells when treated with Crizotinib alone[1]. Cell Viability Assay[1] Cell Line: SW48 isogenic parental or KRAS G12D cells

[1]. Ana J Narvaez, et al. Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7.

Chemical Properties

Cas No. 683808-78-8 SDF
Canonical SMILES O=C(O)CCC1=CC=C(C2=CC=C(Br)C=C2)N1C3=CC=CC=C3C(F)(F)F
Formula C20H15BrF3NO2 M.Wt 438.24
Solubility Storage
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2819 mL 11.4093 mL 22.8185 mL
5 mM 0.4564 mL 2.2819 mL 4.5637 mL
10 mM 0.2282 mL 1.1409 mL 2.2819 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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