Molecular Formula | C17H14Br3N5OS |
Molar Mass | 576.10296 |
Storage Condition | 2-8℃ |
In vitro study | PTC-209 inhibition of UTR-mediated reporter gene expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 reduced the growth of colorectal cancer tumor cells in a BMI-1-dependent manner. In addition, PTC-209 of colorectal cancer-initiating cells (CICs) were damaged by irreversible growth inhibition. |
In vivo study | In primary human colon cancer xenograft, human colon cancer cell line LIM1215 or HCT116 xenograft mice, PTC-209 (60 mg/kg/day, subcutaneous injection) effectively inhibited BMI-1 production in tumor tissue, and to stop the growth of the tumor has been generated. PTC-209 will also reduce the frequency of functional colorectal cancer CICs in vivo. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.736 ml | 8.679 ml | 17.358 ml |
5 mM | 0.347 ml | 1.736 ml | 3.472 ml |
10 mM | 0.174 ml | 0.868 ml | 1.736 ml |
5 mM | 0.035 ml | 0.174 ml | 0.347 ml |
Biological activity | PTC-209 HBr is a PTC-209 hydrobromide, which is a potent selective BMI-1 inhibitor with an IC50 of 0.5 μM, which can irreversibly reduce cancer initiation cells (CICs). |
In vitro study | PTC-209 inhibit UTR-mediated reporter gene expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 reduce the growth of colorectal cancer tumor cells in a BMI-1-dependent manner. In addition, PTC-209 damage colorectal cancer initiation cells (CICs) through irreversible growth inhibition. |
in vivo study | in mice xenograft of primary human colon cancer, human colon cancer cell line LIM1215 or HCT116 xenograft, PTC-209 (60 mg/kg/day, subcutaneous injection) effectively inhibits the production of BMI-1 in tumor tissue and stops the growth of the produced tumor. PTC-209 will also reduce the frequency of functional colorectal cancer CICs in vivo. |
features | BMI-1-selective inhibitor, targeting the BMI-1 self-replication mechanism. |