For research use only.
Molecular Weight(MW): 576.10
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).
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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.
Purity & Quality Control
Choose Selective BMI-1 Inhibitors
|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.|
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. 
|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. |
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.
|In vitro||DMSO||100 mg/mL warmed (173.58 mM)|
|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.
In vivo Formulation Calculator (Clear solution)
|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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
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