Name: PTC-209
Brand: Selleck Chemicals
SKU: S7372
Availability: InStock
Rating: 5 (26 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.99

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other BMI-1 Inhibitors	PTC-209 HBr Unesbulin (PTC596) PTC-028

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (199.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.31mM)	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 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (12.12mM)	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.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Chemical Information, Storage & Stability

Molecular Weight	495.19	Formula	C₁₇H₁₃Br₂N₅OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	315704-66-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br

Mechanism of Action

Features	BMI-1-selective inhibitor targeting self-renewal of cancer cells.
Targets/IC₅₀/Ki	BMI-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. This compound decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, it impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition.
Kinase Assay	Untranslated region-mediated luciferase reporter expression
Kinase Assay	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 this compound.
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. This compound also reduces the frequency of functional colorectal CICs in vivo.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24292392/

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PTC-209 BMI-1 inhibitor

Chemical Structure

Molecular Weight: 495.19