PTC-209

Catalog No.S7372 Batch:S737201

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Technical Data

Formula

C17H13Br2N5OS
Molecular Weight 495.19 CAS No. 315704-66-6
Solubility (25°C)* In vitro DMSO 99 mg/mL (199.92 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
6.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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).
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]
Features BMI-1-selective inhibitor targeting self-renewal of cancer cells.

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[1]
  • 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.
Animal Study:[1]
  • 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.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2017, doi: 10.18632/oncotarget.18002]

Selleck's PTC-209 has been cited by 27 publications

Alpha-tocopherol enhances spermatogonial stem cell proliferation and restores mouse spermatogenesis by up-regulating BMI1 [ Front Nutr, 2023, 10:1141964] PubMed: 37139440
PIC recruitment by synthetic reader-actuators to polycomb-silenced genes blocks triple-negative breast cancer invasion [ bioRxiv, 2023, 2023.01.23.525196] PubMed: 36747762
BMI1 promotes spermatogonial stem cell maintenance by epigenetically repressing Wnt10b/β-catenin signaling [ Int J Biol Sci, 2022, 18(7):2807-2820] PubMed: 35541907
BMI1 nuclear location is critical for RAD51-dependent response to replication stress and drives chemoresistance in breast cancer stem cells [ Cell Death Dis, 2022, 13(2):96] PubMed: 35110528
PRC1-independent binding and activity of RYBP on the KSHV genome during de novo infection [ PLoS Pathog, 2022, 18(8):e1010801] PubMed: 36026503
BMI1 promotes osteosarcoma proliferation and metastasis by repressing the transcription of SIK1 [ Cancer Cell Int, 2022, 22(1):136] PubMed: 35346195
BMI-1 promotes breast cancer proliferation and metastasis through different mechanisms in different subtypes [ Cancer Sci, 2022, 10.1111/cas.15623] PubMed: 36285479
SPP1 Derived from Macrophages Is Associated with a Worse Clinical Course and Chemo-Resistance in Lung Adenocarcinoma [ Cancers (Basel), 2022, 14(18)4374] PubMed: 36139536
The Systematic Analyses of RING Finger Gene Signature for Predicting the Prognosis of Patients with Hepatocellular Carcinoma [ J Oncol, 2022, 2022:2466006] PubMed: 36199791
BMI1 governs the maintenance of mouse GC-2 cells through epigenetic repression of Foxl1 transcription [ Am J Transl Res, 2022, 14(5):3407-3418] PubMed: 35702123

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.