Table 2.
IC50 Summary of Small Molecule Inhibitor Leads
| Compound | Displacement Assay IC50 (µM) | LNCaP IC50 (µM) | DU145 IC50 (µM) | NIH3T3 IC50 (µM) | Patient-Derived Fibroblast IC50 (µM) | HPNE IC50 (µM) | PANC-1 IC50 (µM) | 293T IC50 (µM) |
|---|---|---|---|---|---|---|---|---|
| D13 | 2.98 | 4.84 | 6.45 | 11.48 | 9.1 | 9.145 | 10.19 | 5.7 |
| D36 | 5.90 | 3.24 | 22.4 | 2.77 | 9.9 | 2.65 | 2.52 | 4.3 |
| D90 | 11.7 | 13.8 | 8.68 | 3.80 | 14.4 | 6.54 | 8.36 | 14.7 |
| D58 | 19.6 | N/A | ∼318 | N/A | N/A | N/A | N/A | N/A |
| D7 | N/A | N/A | N/A | 13.91 | 67.1 | 15 | 32.77 | 49.9 |
IC50s of lead compounds in the displacement assay (second column) and growth inhibition assays are summarized. Compounds (first column) were tested in prostate cancer cell lines (LNCaP, DU145), fibroblasts (NIH3T3, patient-derived), and pancreatic cancer cell lines (HPNE, PANC-1) and in 293T. Some IC50s were indeterminably high (displacement assay and growth inhibition assays for LNCaP and DU145); D58 was not examined in NIH3T3, patient-derived fibroblasts, HPNE, PANC-1, and 293T. N/A, data not available.