Биологическая активность
SRX 3305 is a мощный, triple BTK/PI3K/BRD4 ингибитор с IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 с IC50 of 77 and 95 nM.SRX3305 showed enhanced связывание to the препарат-resistant C481S mutant of BTK compared to SRX-3262 (IC50=9 uM and 25 uM, respectively).SRX3305 displayed cytotoxicity aginst MCL клетка lines JeKo-1, Mino, Granta с IC50 of 58 nM, 1 nM, 1.1 uM, respectively.SRX3305 inhibited клетка vbiability of JeKo-1 BTK C481S and Mino BTK C481S mutant клетка lines с IC50 of 1 uM and 47 nM, respectively, with minimally toxic to healthy donor PBMCs.SRX3305 showed improved efficacy in MCL and Ibrutinib-resistant MCL cells, SRX3305 impacted gene expression, perturbs the клетка cycle and promotes apoptosis in MCL.
Оригинал на английском
SRX 3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.SRX3305 showed enhanced binding to the drug-resistant C481S mutant of BTK compared to SRX-3262 (IC50=9 uM and 25 uM, respectively).SRX3305 displayed cytotoxicity aginst MCL cell lines JeKo-1, Mino, Granta with IC50 of 58 nM, 1 nM, 1.1 uM, respectively.SRX3305 inhibited cell vbiability of JeKo-1 BTK C481S and Mino BTK C481S mutant cell lines with IC50 of 1 uM and 47 nM, respectively, with minimally toxic to healthy donor PBMCs.SRX3305 showed improved efficacy in MCL and Ibrutinib-resistant MCL cells, SRX3305 impacted gene expression, perturbs the cell cycle and promotes apoptosis in MCL.
Химические свойства
- CAS №
- 2409965-28-0
- Брутто-формула
- C₂₂H₂₀N₂O₅S
- Мол. масса
- 424.47 г/моль
- Синонимы
- SRX 3305
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО Publication: 1. Kendra R Vann, et al. Mol Biomed. 2022 Jan 15;3(1):2
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.