PDGFR-IN-1 is an orally active, highly efficient platelet-derived growth factor receptor (PDGFR) inhibitor with potent antitumor activity. It inhibits PDGFRα and PDGFRβ and can be used in solid tumor research.

PDGFRβ:0.9 nM, PDGFRα:2.4 nM

PDGFR-IN-1 is a potent inhibitor of PDGFR (platelet-derived growth factor receptor) with IC50 of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively.
PDGFR-IN-1 showed the highest antiproliferative activity against human osteosarcoma cancer cell lines with abnormal PDGFRα and/or PDGFRβ activation (MG63, U2OS, MNNG/HOS, and SAOS-2). The IC50 values were 0.44, 0.42, 1.03 and 0.37 μM, respectively.
PDGFR-IN-1 (0.1, 0.2, and 0.4 μM) inhibited α-tubulin expression IN MNNG/HOS and MG63 cells in a dose-dependent manner, thereby inhibiting cancer cell formation.
PDGFR-IN-1 inhibits PDGFRβ phosphorylation and downstream signal transduction (p-STAT3, p-AKT, and p-ERK) IN MNNG/HOS cells.
PDGFR-IN-1 significantly inhibits the migration and invasion of osteosarcoma cancer cells by down-regulating the expression of FAK and its distribution on the cell front. [1]

Orally administered PDGFR-IN-1 (40, 80 mg/kg/ day for 10 days), the mice showed good resistance.
IN a MNNG/HOS xenograft mouse model, PDGFR-IN-1 (30 mg/kg for 14 days) treatment significantly inhibited tumor growth. [1]