| Bioactivity | PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma[1]. |
| Invitro | PDGFR-IN-1 (compound 7m) (0-0.4 μM, 48 h) inhibits osteosarcoma cancer cells (U2OS, MG63, MNNG/HOS, and SAOS-2) proliferation and colony formation[1].PDGFR-IN-1 (0-0.4 μM, 48 h) induces cell-cycle arrest in a dose-dependent manner[1].PDGFR-IN-1 (0-1.6 μM, 48 h) induces MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner[1].PDGFR-IN-1 (0-0.4 μM, 15 min) inhibits the expression of α-tubulin in both MNNG/HOS and MG63 cells[1].PDGFR-IN-1 (0-0.4 μM, 48 h) inhibits PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK)[1].PDGFR-IN-1 (0-0.4 μM, 48 h) significantly inhibits osteosarcoma cancer cell migration and invasion by downregulating the expression of FAK, as well as the distribution in the leading edge of cells[1]. Cell Proliferation Assay Cell Line: |
| Name | PDGFR-IN-1 |
| CAS | 2644673-07-2 |
| Formula | C25H30N8O |
| Molar Mass | 458.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |