PTC-209 NEW
Price | $68 | $117 | $441 |
Package | 5mg | 10mg | 50mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: PTC-209 | CAS No.: 315704-66-6 |
Purity: 99.60% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | PTC-209 |
Description | PTC-209 is a potent and selective BMI-1 inhibitor. |
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) |
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. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : 9.9 mg/mL (20 mM) DMSO : 50 mg/mL (100.97 mM), Sonication is recommended. |
Keywords | tumor | PTC-209 | lung | Inhibitor | inhibit | HEK293T | colon | CICs | cells | cancer-initiating | breast | Autophagy | anti-myeloma |
Inhibitors Related | Stavudine | Aceglutamide | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Valproic Acid | Curcumin | Paeonol | Naringin | Salicylic acid | Gefitinib |
Related Compound Libraries | Anti-Colorectal Cancer Compound Library | DNA Damage & Repair Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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