Биологическая активность
PD-161570 is a селективный FGFR ингибитор (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 рецептор (IC50 = 40 nM) compared with the PDGFbeta рецептор (IC50 = 262 nM) or EGF рецептор (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed constitutive phosphorylation of the FGF-1 рецептор in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 рецептор and blocked the growth of A121(p) cells in culture. The results demonstrate a novel synthetic ингибитор with nanomolar potency and specificity towards the FGF-1 рецептор tyrosine киназы.
Оригинал на английском
PD-161570 is a selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture. The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.
Химические свойства
- CAS №
- 192705-80-9
- Брутто-формула
- C₂₆H₃₅Cl₂N₇O
- Мол. масса
- 532.51 г/моль
- SMILES
- O=C(NC(C)(C)C)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
- Синонимы
- PD-161570; PD 161570; PD161570.
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.