Биологическая активность
PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-препарат resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-BCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in клетка-free assays and causes microtubule depolymerization in MCF-7 cells by связывание a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.
Оригинал на английском
PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-BCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells by binding a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.
Химические свойства
- CAS №
- 290814-68-5
- Брутто-формула
- C₂₅H₂₀N₂O₃
- Мол. масса
- 396.45 г/моль
- SMILES
- O=C(OC1=C(C2=C3C=CC=CC3=CC=C2)OC4=CC=CC=C4N5C1=CC=C5)N(C)C
- Синонимы
- PBOX-6
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.