Home Cell Cycle BMI-1 inhibitor PTC-209 For research use only.

PTC-209

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).

PTC-209 Chemical Structure

PTC-209 Chemical Structure

CAS No. 315704-66-6

Purity & Quality Control

Batch: S737201 DMSO]99 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.99%
99.99

PTC-209 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 0.00065 μM. 30429953
HCT8 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay, IC50 = 0.59 μM. 30429953
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50 = 0.61 μM. 30429953
HCT116 Function assay 8 hrs Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis, IC50 = 0.7 μM. 30429953
HCT116 Function assay 0.1 to 0.4 uM 7 days Inhibition of colony formation in human HCT116 cells at 0.1 to 0.4 uM after 7 days by crystal violet staining based assay 30429953
HCT116 Antitumor assay 10 mg/kg/day 18 days Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as tumor growth inhibition at 10 mg/kg/day, ip for 18 days 30429953
HCT116 Antitumor assay 10 mg/kg/day 18 days Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as reduction in Ki67 expression in tumor at 10 mg/kg/day, ip for 18 days by IHC analysis 30429953
HCT116 Function assay 10 mg/kg/day 18 days Decrease in Bmi1 expression in tumors of nude mouse xenografted with human HCT116 cells at 10 mg/kg/day, ip for 18 days by IHC analysis 30429953
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research 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.

Chemical Information & Solubility

Molecular Weight 495.19 Formula

C17H13Br2N5OS
CAS No. 315704-66-6 SDF Download PTC-209 SDF
Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (199.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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