Биологическая активность
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable лиганд and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-препарат adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and клетка proliferation. Lobaplatin has activity in a wide range of preclinical tumour models and appears to overcome tumour resistance to cisplatin and carboplatin in some of these models. In the body, lobaplatin remains largely intact until removed by glomerular filtration.
Оригинал на английском
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation. Lobaplatin has activity in a wide range of preclinical tumour models and appears to overcome tumour resistance to cisplatin and carboplatin in some of these models. In the body, lobaplatin remains largely intact until removed by glomerular filtration.
Химические свойства
- CAS №
- 135558-11-1
- Брутто-формула
- C₉H₁₈N₂O₃Pt
- Мол. масса
- 395.31 г/моль
- SMILES
- CC1[O-][Pt]2(NCC3C(CC3)CN2)[O-]C1=O
- Синонимы
- Platinum,[rel-(1R,2R)-1,2-cyclobutanedimethanamine-kN,kN'][(2S)-2-(hydroxy-kO)propanoato(2-)-kO]-, (SP-4-3)- (9CI); Platinum, [rel-(1R,2R)-1,2-cyclobutanedimethanamine-.kappa.N,.kappa.N'][(2S)-2-(hydroxy-.kappa.O)propanoato(2-)-.kappa.O]-, (SP-4-3)- (9CI) (CA INDEX NAME); Platinum,[rel-(1R,2R)-1,2-cyclobutanedimethanamine-kN,kN'][(2S)-2-(hydroxy-kO)propanoato(2-)-k...; d19466; Lobaplatin (D-19466) и ещё 2
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.