Биологическая активность
Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate. 17β-Hydroxy exemestane is an aromatase ингибитор (IC50 = 69 nM) and an androgen рецептор (AR) агонист (IC50 = 39.6 nM) that is селективный for AR over estrogen рецептор α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
Оригинал на английском
Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate. 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
Химические свойства
- CAS №
- 1144617-49-1
- Брутто-формула
- C₅₁H₈₈O₆₀S₁₃
- Мол. масса
- 2078.05 г/моль
- SMILES
- C[C@@]12[C@]3([H])[C@](CC[C@@]1([H])C[C@H](CC2)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)COS(=O)(O)=O)O[C@@H]5[C@@H]([C@H]([C@@H]([C@H](O5)COS(=O)(O)=O)O[C@@H]6[C@@H]([C@H]([C@@H]([C@H](O6)COS(=O)(O)=O)O[C@@H]7[C@@H]([C@H]([C@@H]([C@H](O7)COS(=O)(O)=O)OS(=O)(O)
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.