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PT2399 is a potent and orally available antagonist of HIF-2 with an IC50 of 6 nM, PT2399 selectively disrupts the heterodimerization of HIF-2α with HIF-1β. PT2399 dissociates HIF-2 (an obligatory heterodimer [HIF-2α/HIF-1β])14 in human Clear cell Renal Cell Carcinoma (ccRCC) suppressing tumorigenesis in 56% (10/18) lines. PT2399 (20 μM) causes off-target toxicity because it inhibits the proliferation of HIF-2α −/− 786-O cells and other cancer cell lines with undetectable HIF-2α. PT2399 (0.2-2 μM; 0-21 days) inhibits 786-O cells soft agar growth.
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice. PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than SU 11248, and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice.
| Cell Experiment | |
|---|---|
| Cell lines | 786-O cells |
| Preparation method | PT2399 inhibited 786-O cell soft agar growth at 0.2-2 μM. |
| Concentrations | 0 μM, 0.2 μM, 2 μM |
| Incubation time | 0-21 days |
| Animal Experiment | |
|---|---|
| Animal models | Mice with RCC tumorgraft |
| Formulation | in 10% EtOH, 30% PEG400, 60% MCT |
| Dosages | 100 mg/kg |
| Administration | oral gavage every 12 hours |
| Molecular Weight | 419.32 |
| Formula | C17H10F5NO4S |
| CAS Number | 1672662-14-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | -20°C, sealed |
[3] Wenfang Chen, et al. Nature. Targeting renal cell carcinoma with a HIF-2 antagonist
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