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PTC-209

Catalog No. T2345 CAS 315704-66-6

Synonyms: PTC209, PTC 209

PTC-209 is a potent and selective BMI-1 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PTC-209, CAS 315704-66-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 47.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
50 mg	In stock	$ 441.00
100 mg	In stock	$ 451.00

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Purity: 99.60%

Purity: 99.52%

Purity: 99.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PTC-209 is a potent and selective BMI-1 inhibitor.
Targets&IC50	BMI1:0.5 μM
In vitro	PTC-209 effectively reduces the frequency of functional colorectal cancer cancer-initiating cells (CICs) in vivo. Administered at a dosage of 60 mg/kg/day subcutaneously (s.c.), PTC-209 significantly inhibits the production of BMI-1 in tumor tissues and halts the growth of pre-established tumors in mice with primary human colorectal cancer xenografts, as well as in xenografts from human colorectal cancer cell lines LIM1215 or HCT116.
In vivo	PTC-209 irreversibly inhibits the growth of colorectal cancer initiating cells (CIC) by targeting BMI-1, resulting in the destruction of these cells. It suppresses UTR-mediated reporter gene expression and endogenous BMI-1 expression in human colorectal HCT116 cells and human fibrosarcoma HT1080 tumor cells. Furthermore, PTC-209 reduces the growth of rectal tumor cells in a BMI-1 dependent manner.
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	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.(Only for Reference)

Synonyms	PTC209, PTC 209
Molecular Weight	495.19
Formula	C17H13Br2N5OS
CAS No.	315704-66-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 9.9 mg/mL (20 mM)

DMSO: 49.5 mg/mL (100 mM)

References and Literature

1. Kreso A, et al. Nat Med. 2014, 20(1), 29-36.

Citations

1. Xu J, Zhang Y, Xu J, et al. Reversing tumor stemness via orally targeted nanoparticles achieves efficient colon cancer treatment. Biomaterials. 2019: 119247.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Cell Cycle Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max DNA Damage & Repair Compound Library Target-Focused Phenotypic Screening Library Autophagy Compound Library Anti-Colorectal Cancer Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets

PTC-028 PRT4165 XMD8-92 PTC-209 hydrobromide Unesbulin

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PTC-209 315704-66-6 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair BMI-1 tumor cells inhibit anti-myeloma HEK293T cancer-initiating lung CICs breast PTC209 PTC 209 colon Inhibitor inhibitor

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