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ML 239 (Synonyms: CID49843203)

Catalog No.GC17468 Copy One-Click Copy Product Info

Le ML 239 est un inhibiteur puissant et sélectif des cellules souches du cancer du sein, avec une IC50 de 1,16 μM.

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ML 239 Chemical Structure

Cas No.: 1378872-36-6

Taille Prix Stock Qté
10mg
81,00 $US
Ship Within 40 Days
50mg
305,00 $US
Ship Within 40 Days

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Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of ML 239

ML239 is the best-in-class inhibitor of the breast cancer stem cells with an IC50 = 1.16 µM. [1]

ML239 was a selective inhibitor an IC50= 1.18 µM against HMLE_sh_ECad, demonstrated a >23-fold selectivity over the control line, and was toxic to another CSC-like line, HMLE_shTwist, and a breast carcinoma cell line, MDA-MB-231. Five genes (ATP6V0C, PKM2, PPDPF, RPL23, and SERINC2) were differentially regulated in HMLE_sh_GFP after treatment with ML239. Gene expression studies conducted with ML239-treated cells showed altered gene expression in the NF-κB pathway in the HMLE_sh_ECad line but not in the isogenic control line. ML239 was selectively toxic toward another CSC-like cell line, HMLE_Twist, and the breast cancer line, MDA-MB-231. Similar to the results observed in the HMLE_sh_ECad cell line, ML239 was potently toxic, inhibiting HMLE_Twist with an IC50 ~0.1 µM. ML239 displayed potent toxicity (IC50 = 2.81 µM) to the breast carcinoma cell line, MDA-MB-231 [1]. ML239 also alters the expression of genes in the NF-κB, MAPK and inflammatory cytokine pathways.

 

Reference:

1.Phenotypic high-throughput screening elucidates target pathway in breast cancer stem cell-like cells. J Biomol Screen. 2012 Oct;17(9):1204-10. Epub 2012 Aug 30.

Protocol of ML 239

Cell experiment:

Cancer cell lines (CCLs) are plated at a density of 500 cells/well in white opaque tissue-culture-treated Aurora 1536-well MaKO plates in the provider-recommended growth media using a highly automated platform. Compounds (ML239) are added by acoustic transfer using a Labcyte Echo 555. 24 hours after plating. The effects of small molecules (ML239) are measured over a 16-point concentration range (two-fold dilution) in duplicate. DMSO is used at a constant concentration of 0.33%, including vehicle-only control wells. As a surrogate for viability, cellular ATP levels are assessed 72 hours after compound transfer by addition of CellTiterGlo followed by luminescence measurement using a ViewLux Microplate Imager. Duplicates are averaged and luminescence values normalized to vehicle (DMSO) treatment and background (media-only) wells[2].

References:

[1]. Germain AR, et al. Identification of a selective small molecule inhibitor of breast cancer stem cells. Bioorg Med Chem Lett. 2012 May 15;22(10):3571-4.
[2]. Rees MG, et al. Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016 Feb;12(2):109-16.

Chemical Properties of ML 239

Cas No. 1378872-36-6 SDF
Synonymes CID49843203
Chemical Name (1Z,N'E)-N'-((1H-pyrrol-2-yl)methylene)-2-(2,4,6-trichlorophenoxy)acetohydrazonic acid
Canonical SMILES ClC1=CC(Cl)=C(OC/C(O)=N/N=C([H])/C2=CC=CN2)C(Cl)=C1
Formula C13H10Cl3N3O2 M.Wt 346.6
Solubility DMSO: 10 mg/ml Storage Store at -20°C
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 of ML 239

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1 mg 5 mg 10 mg
1 mM 2.8852 mL 14.4259 mL 28.8517 mL
5 mM 577 μL 2.8852 mL 5.7703 mL
10 mM 288.5 μL 1.4426 mL 2.8852 mL
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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 saline, mix and clarify.

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

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for ML 239

Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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