PTC-209 HBr

For research use only.

Catalog No.S7539

10 publications

PTC-209 HBr Chemical Structure

CAS No. 1217022-63-3

PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).

Selleck's PTC-209 HBr has been cited by 10 publications

3 Customer Reviews

  • b Reduced viability 96 h post treatment was observed in all MM cell lines in a dose-dependent manner, but not in BMSCs or PBMCs (c). d Downregulation of CCND1 and MYC as well as upregulation of CDNK1A and CDKN1B was noted 5 h post treatment. e Deregulation of proliferation-associated genes translated into a significant increase of cells in the G1 phase and concurrent decrease in the S and G2M phase of the cell cycle 24 h post treatment. ***P < 0.001, **P < 0.01 and *P < 0.05 vs DMSO control

    J Hematol Oncol, 2016, 9:17. PTC-209 HBr purchased from Selleck.

    C. Western blot images of GBC cells treated with 1.25 μM PTC-209 for 72 h (n = 4, cropped). Abbreviations: BMI1: BMI1 polycomb ring finger oncogene; h: hours; H2AK119ub: mono-ubiquitylation of histone 2A at lysine 119; PRC1: polycomb repressive complex 1; RING1B: ring finger protein 2.

    Oncotarget, 2016, 7(1):745-58. PTC-209 HBr purchased from Selleck.

  • Western blot analysis of U87MG cell lysates following PTC-209 (1 μM and 10 μM) or vehicle control (DMSO) treatment for 4 days.

    Cell Cycle, 2018, 17(10):1199-1211. PTC-209 HBr purchased from Selleck.

Purity & Quality Control

Choose Selective BMI-1 Inhibitors

Biological Activity

Description PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).
Features BMI-1-selective inhibitor, targeting the BMI-1 self-renewal machinery.
BMI-1 [1]
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]


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.
  • Dosages: ~60 mg/kg/day
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (173.58 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+35% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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 576.10


CAS No. 1217022-63-3
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br.Br

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID