Биологическая активность
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen рецептор (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing клетка cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant. BY13 significantly inhibits the growth of препарат-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model.
Оригинал на английском
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant. BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model.
Химические свойства
- Брутто-формула
- C₃₅H₃₅N₉O₄
- Мол. масса
- 645.71 г/моль
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.