Catalog No.GC60294

Poloppin Chemical Structure

Size Price Stock Qty
In stock
In stock

Customer Reviews

Based on customer reviews.

Tel: (626) 353-8530 Email: sales@glpbio.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:


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
Synonyms N/A
Chemical Name N/A
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 N/A Storage N/A
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

  • Molarity Calculator

  • Dilution Calculator

**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).



Review for Poloppin

Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

5 Star
4 Star
3 Star
2 Star
1 Star
Review for Poloppin

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.