PTC-209 hydrobromide
Based on 16 publication(s) in Google Scholar
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
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- Pureté: 99.02%
- CAS No.: 1217022-63-3
- Formule: C17H14Br3N5OS
- Masse moléculaire:576.10
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) PTC-209 hydrobromide
More- Cell Stem Cell. 2017 May 4;20(5):621-634.e6. [Abstract]
- Adv Funct Mater. 2024 Oct 04.
- Nat Commun. 2018 Feb 5;9(1):500. [Abstract]
- ACS Nano. 2025 Apr 1;19(12):12237-12252. [Abstract]
- Cell Rep Med. 2025 Apr 8:102077. [Abstract]
- Pharmacol Res. 2021 Feb:164:105365. [Abstract]
- Mater Today Bio. 2025 Mar 29:32:101721. [Abstract]
- Acta Biomater. 2023 Oct 15:170:273-287. [Abstract]
- Oncogene. 2020 Jan;39(1):17-29. [Abstract]
- Apoptosis. 2015 Jan;20(1):75-82. [Abstract]
- Cancers (Basel). 2022 Dec 1;14(23):5947. [Abstract]
- J Biomed Mater Res A. 2025 Apr;113(4):e37909. [Abstract]
- Stem Cells Int. 2020 Aug 20;2020:8877577. [Abstract]
- Front Oncol. 2021 Mar 22:11:620295. [Abstract]
- Anticancer Res. 2024 Dec;44(12):5283-5292. [Abstract]
- University of Glasgow. 2022.
Customer Validation & Images
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Activité biologique
IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]
PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
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Concentration:0.01-10 µM
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Incubation Time:24, 48, and 72 hour
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Result:Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
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Dosage:60 mg/kg body weight
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Administration:Subcutaneously; once a day for 11 days
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Result:Significantly reduced tumor volume.
Chemical Information
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CAS No. 1217022-63-3
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Appearance Solid
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Masse moléculaire 576.10
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Formule C17H14Br3N5OS
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Color Light yellow to yellow
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SMILES
CC1=C(C2=CSC(NC3=C(Br)C=C(OC)C=C3Br)=N2)N4C=CC=NC4=N1.Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (16)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Targeting BMI1+ Cancer Stem Cells Overcomes Chemoresistance and Inhibits Metastases in Squamous Cell Carcinoma. [Abstract]2017 May 4;20(5):621-634.e6. PMID: 28285905
PTC-209 hydrobromide purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2017 May 4;20(5):621-634.e6. [Abstract]
The Combination Therapy of Cisplatin Plus PTC-209 Potently Eradicates Bmi1+ CSCs and Inhibits Tumor Progression by Lineage Tracing. Western blots show that Bmi1 is reduced in tumors treated with PTC-209.
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Nat Commun
BMI1 regulates androgen receptor in prostate cancer independently of the polycomb repressive complex 1. [Abstract]2018 Feb 5;9(1):500. PMID: 29402932
PTC-209 hydrobromide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Feb 5;9(1):500. [Abstract]
BMI1-specific antagonist inhibits androgen receptor (AR)-signaling pathway. C4-2 or 22Rv1 is treated with PTC209 in indicated concentration for 48 h, BMI1 and AR are tested by western blot, and GAPDH served as loading control.
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ACS Nano
A Hybrid Manganese Nanoparticle Simultaneously Eliminates Cancer Stem Cells and Activates STING Pathway to Potentiate Cancer Immunotherapy. [Abstract]2025 Apr 1;19(12):12237-12252. PMID: 40116158 -
Cell Rep Med
2025 Apr 8:102077. PMID: 40239645 -
Pharmacol Res
Bmi1 drives the formation and development of intrahepatic cholangiocarcinoma independent of Ink4A/Arf repression. [Abstract]2021 Feb:164:105365. PMID: 33307220 -
Mater Today Bio
CD44-targeted virus-mimicking nanomedicine eliminates cancer stem cells and mitigates chemoresistance in head and neck squamous cell carcinoma. [Abstract]2025 Mar 29:32:101721. PMID: 40242481 -
Acta Biomater
Core-Shell Cisplatin/SiO2 Nanocapsules Combined with PTC-209 Overcome Chemotherapy-Acquired and Intrinsic Resistance in Hepatocellular Carcinoma. [Abstract]2023 Oct 15:170:273-287. PMID: 37597681 -
Oncogene
BMI1 is directly regulated by androgen receptor to promote castration-resistance in prostate cancer. [Abstract]2020 Jan;39(1):17-29. PMID: 31462713
PTC-209 hydrobromide purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Jan;39(1):17-29. [Abstract]
BMI1 inhibitor delays CRPC progression in vivo. C4-2 cells are treated with PTC209.
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Apoptosis
MiR-218-targeting-Bmi-1 mediates the suppressive effect of 1,6,7-trihydroxyxanthone on liver cancer cells. [Abstract]2015 Jan;20(1):75-82. PMID: 25416134 -
Cancers (Basel)
Glucose and Cell Context-Dependent Impact of BMI-1 Inhibitor PTC-209 on AKT Pathway in Endometrial Cancer Cells. [Abstract]2022 Dec 1;14(23):5947. PMID: 36497428 -
J Biomed Mater Res A
Targeting Dysregulated Epigenetic Modifiers With Kidney-Targeted Nanotherapeutics for Polycystic Kidney Disease. [Abstract]2025 Apr;113(4):e37909. PMID: 40200735 -
Stem Cells Int
Bmi1 Severs as a Potential Tumor-Initiating Cell Marker and Therapeutic Target in Esophageal Squamous Cell Carcinoma. [Abstract]2020 Aug 20;2020:8877577. PMID: 32884573 -
Front Oncol
2021 Mar 22:11:620295. PMID: 33828977 -
Anticancer Res
Resveratrol Can Differentiate Human Melanoma Stem-like Cells from Spheroids Treated With All-trans Retinoic Acid. [Abstract]2024 Dec;44(12):5283-5292. PMID: 39626925 -
Solvant et solubilité
DMSO : 100 mg/mL (173.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.34 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.34 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36. [Content Brief]
[2]. Christian Mayr, et al. The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Oncotarget. 2016 Jan 5; 7(1): 745-758. [Content Brief]
[3]. Shahi MH, et al. BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance. PLoS One. 2015 Jun 25;10(6):e0131006. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7358 mL | 8.6790 mL | 17.3581 mL | 43.3952 mL |
| 5 mM | 0.3472 mL | 1.7358 mL | 3.4716 mL | 8.6790 mL | |
| 10 mM | 0.1736 mL | 0.8679 mL | 1.7358 mL | 4.3395 mL | |
| 15 mM | 0.1157 mL | 0.5786 mL | 1.1572 mL | 2.8930 mL | |
| 20 mM | 0.0868 mL | 0.4340 mL | 0.8679 mL | 2.1698 mL | |
| 25 mM | 0.0694 mL | 0.3472 mL | 0.6943 mL | 1.7358 mL | |
| 30 mM | 0.0579 mL | 0.2893 mL | 0.5786 mL | 1.4465 mL | |
| 40 mM | 0.0434 mL | 0.2170 mL | 0.4340 mL | 1.0849 mL | |
| 50 mM | 0.0347 mL | 0.1736 mL | 0.3472 mL | 0.8679 mL | |
| 60 mM | 0.0289 mL | 0.1447 mL | 0.2893 mL | 0.7233 mL | |
| 80 mM | 0.0217 mL | 0.1085 mL | 0.2170 mL | 0.5424 mL | |
| 100 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.4340 mL |
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