Биологическая активность
SJ432 (SJ-432) is a мощный, highly селективный BET BD2 ингибитор with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).SJ432 potently inhibits MV4-11 клетка growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB клетка lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.
Оригинал на английском
SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.
Химические свойства
- CAS №
- 2230677-55-9
- Брутто-формула
- C₂₂H₂₁N₅O
- Мол. масса
- 371.44 г/моль
- SMILES
- C1(N[C@H]2C3=CC(C4C=CNN=4)=CC=C3N(C(C)=O)[C@H](C2)C)C=CC(=CC=1)C#N
- Синонимы
- SJ432; 4-[[(2S,4R)-1-Acetyl-1,2,3,4-tetrahydro-2-methyl-6-(1H-pyrazol-3-yl)-4-quinolinyl]amino]benzonitrile; SJ 432
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.