PTC-209

Catalog No.S7372

PTC-209 Chemical Structure

Molecular Weight(MW): 495.19

PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).

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Cited by 4 Publications

1 Customer Review

  • Immunoblot analysis of BMI-1 and H2AK119Ub levels following 72 h treatment with 10 µM PTC-209. β-actin and total H2A served as loading controls.

    Oncotarget, 2017, doi: 10.18632/oncotarget.18002. PTC-209 purchased from Selleck.

Purity & Quality Control

Choose Selective BMI-1 Inhibitors

Biological Activity

Description PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
Features BMI-1-selective inhibitor targeting self-renewal of cancer cells.
Targets
BMI-1 [1]
(HEK293T cells)
0.5 μM
In vitro

PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1]

In vivo PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1]

Protocol

Kinase Assay:[1]
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Untranslated region-mediated luciferase reporter expression:

HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control.
Cell Research:[1]
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  • Cell lines: Human lymphoma U937 and HT1080 tumor cells, primary human peripheral blood mononuclear cells and human hematopoietic stem cells.
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Primary human colon cancer xenograft, human colon cancer cell lines LIM1215 and HCT116 xenografts in nude mice.
  • Formulation: 14% DMSO, 36% polyethylene glycol 400 and 50% polypropylene glycol.
  • Dosages: ~60 mg/kg/day
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL (199.92 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 495.19
Formula

C17H13Br2N5OS

CAS No. 315704-66-6
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID