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CP 673451 is a pharmacologically selective PDGFR-beta inhibitor and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells (IC50 = 1 nmol/L) being more than 450-fold selective for PDGFR-beta versus other angiogenic receptors. Inhibition of PDGFR-beta phosphorylation in tumors correlates with plasma and tumor levels of CP673451. A dose of 33 mg/kg was adequate to provide >50% inhibition of receptor for 4 hours corresponding to an EC50 of 120 ng/mL in plasma at C(max). In a sponge angiogenesis model, CP 673451 inhibited 70% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg (q.d. x 5, p.o., corresponding to 5.5 ng/mL at C(max)). In vivo, CP 673451 inhibits tumor PDGFR-beta phosphorylation, and it also selectively inhibits PDGF-BB-stimulated angiogenesis. CP 673451 causes significant tumor growth inhibition in multiple human xenograft models.
| Cell Experiment | |
|---|---|
| Cell lines | H526 small cell lung cancer cells |
| Preparation method | For both assays, cells were starved overnight and treated the following day with increasing concentrations of CP-673,451 for 30 minutes at 37°C. During the final 5 to 8 minutes of incubation, either stem cell factor (50 ng/mL) or PDGF-BB (500 ng/mL) was added. Unstimulated cells were used as phosphorylation controls. Cells were washed, lysed, and equivalent protein levels were separated by PAGE. Following transfer to nitrocellulose, membranes were blotted to detect phospho-PDGFR (pY857 antibody) or phospho-c-kit (pY719 antibody) antibody at 1: 200 overnight at 4°C. Densitometry of bands and IC50 calculation were measured using a LumiImager. |
| Concentrations | 0~3000 n M |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing Colo205 tumors xenograft model |
| Formulation | 5% Gelucire |
| Dosages | 10, 33, and 100 mg/kg twice daily for 10 days |
| Administration | oral gavage |
| Molecular Weight | 417.5 |
| Formula | C24H27N5O2 |
| CAS Number | 343787-29-1 |
| Solubility (25°C) | DMSO 32 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Nintedanib
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