PTC-209 hydrobromide

SKU: orb1688258

Description

PTC-209 hydrobromide is the salt form of a potent, selective BMI-1 inhibitor (IC50 = 0.5 µM). It irreversibly diminishes cancer-initiating cell populations and has been applied in both in vitro and in vivo oncology research to study stemness and tumorigenesis.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1217022-63-3
• MW: 576.1
• Purity: 99.91%
• Formula: C₁₇H₁₃Br₂N₅OS·HBr
• SMILES: Br.COC1=CC(Br)=C(NC2=NC(=CS2)C2=C(C)N=C3N=CC=CN23)C(Br)=C1
• Target: Autophagy,BMI-1
• Solubility: DMSO:93 mg/mL (161.43 mM);H2O:<1 mg/mL;10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.73 mM);Ethanol:<1 mg/mL

Bioactivity

• Target IC50:
  BMI1:0.5 μM
• 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.
• 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. 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.
• 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)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cells, colon, breast, CICs, Autophagy, anti-myeloma, cancer-initiating, BMI-1, BMI1, Inhibitor, HEK293T, lung, inhibit, PTC209, PTC-209, PTC-209 HBr, PTC209 Hydrobromide, PTC209 hydrobromide, PTC-209 Hydrobromide, PTC 209, PTC 209 Hydrobromide, PTC 209 hydrobromide, tumor

Compound Identifiers

PubChem CID

76458124