Name | PD 161570 |
Synonyms | PD-161570 PD 161570 PF-1480232 PD-161570 PF-1480232 1-(tert-Butyl)-3-(6-(2,6-dichlorophenyl)-2-((4-(diethylamino)butyl)amino)pyrido[2,3-d]pyrimidi 1-Tert-butyl-3-[6-(2,6-dichloro-phenyl)-2-(4-diethylaMino-butylaMino)pyrido[2,3-d]pyriMidin-7-yl]urea N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea |
CAS | 192705-80-9 |
Molecular Formula | C26H35Cl2N7O |
Molar Mass | 532.51 |
Melting Point | 215-230?C |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | white to off-white |
Storage Condition | Store at RT |
MDL | MFCD16618403 |
In vitro study | PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC 50 of 0.3 µM on day 8. PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A 121(p) ) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A 121(p) cells in culture. PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis. Cell Proliferation Assay Cell Line: Vascular smooth muscles cells (VSMCs) Concentration: 0.1 µM, 0.3 µM, 1 µM Incubation Time: 1 day, 3 days, 6 days, 8 days Result: Inhibited VSMC proliferation in a dose dependent fashion with an IC 50 of 0.3 µM at day 8. |
Hazard Symbols | T - Toxic |
Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
biological activity | PD-161570 is an effective and ATP-competitive human FGF-1 receptor inhibitor, IC50 is 39.9 nM,Ki is 42 nM. PD-161570 also inhibited PDGFR,EGFR and c-Src tyrosine kinase with IC50 values of 310 nM,240 nM and 44 nM, respectively. PD-161570 inhibit PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50 of 450 nM and 622 nM, respectively. PD-161570 is also an inhibitor of bone morphogenetic proteins (BMPs) and TGF-β signaling. |
target | FGFR1 39.9 nM (IC 50 ) FGFR1 42 nM (Ki) FGFR1 autophosphorylation 622 nM (IC 50 ) PDGFRβ 262 nM (IC 50 ) PDGFR 310 nM (IC 50 ) EGFR 240 nM (IC 50 ) c-Src 44 nM (IC 50 ) TGF-β Receptor |
in vitro study | PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC 50 of 0.3 m on day 8. PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A 121(p) ) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of a 121(p) cells in culture. PD-161570 can potently inhibit basic fibroblast growth factor (BFGF)-mediated angiogenesis. Cell Proliferation Assay Cell Line: vascular smooth muscles cells (VSMCs) Concentration: 0.1 m, 0.3 m, 1 m Incubation time: 1 day, 3 days, 6 days, 8 days result: Inhibited VSMC proliferation in a dose dependent fashion with an IC 50 of 0.3 m at day 8. |
Cell Line: | Vascular smooth muscles cells (VSMCs) |
Concentration: | 0.1 µM, 0.3 µM, 1 µM |
Incubation Time: | 1 day, 3 days, 6 days, 8 days |
Result: | Inhibited VSMC proliferation in a dose dependent fashion with an IC 50 of 0.3 µM at day 8. |