PTC-209

SKU: orb1305632

Description

PTC-209

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 315704-66-6
• MW: 495.19
• Purity: 99.43%
• Formula: C₁₇H₁₃Br₂N₅OS
• SMILES: COc1cc(Br)c(Nc2nc(cs2)-c2c(C)nc3ncccn23)c(Br)c1
• Target: BMI-1,Autophagy
• Solubility: Ethanol:9.9 mg/mL (19.99 mM);DMSO:50 mg/mL (100.97 mM)

Bioactivity

• Target IC50:
  BMI1:0.5 μM
• In Vivo:
  PTC-209 irreversibly inhibit 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 reduce the growth of rectal tumor cells in a BMI-1 dependent manner.
• In Vitro:
  PTC-209 effectively reduce 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 inhibit the production of BMI-1 in tumor tissues and halt 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.
• Cell Research:
  To determine whether pretreatment wit the inhibitor affects tumor cell growth, cells are plated wit 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 evaluatin the number of wells containing spheres. Fo 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 followin the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal o the drug. Long-lasting effects o 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) usin the cells obtained 120 h afte the 4-d drug treatment.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

1117196