2306193-61-1
中文名稱
VZ185
英文名稱
VZ185
CAS
2306193-61-1
分子式
C53H67FN8O8S
更新日期
2023/03/20 15:41:21
分子量
995.21
物理化學(xué)性質(zhì)
沸點(diǎn)1116.1±65.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 200 mg/mL (200.96 mM; Need ultrasonic)
酸度系數(shù)(pKa)13.79±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
VZ185 是高效，快速，選擇性的 BRD7/9 PROTAC 降解劑，DC50 分別為 4.5 和 1.8 nM。VZ185對(duì) EOL-1 和 A-402 細(xì)胞具有細(xì)胞毒性，EC50 分別為 3nM 和 40nM。靶點(diǎn)
|
BRD7 4.5 nM (DC 50 ) |
BRD9 1.8 nM (DC 50 ) |
體外研究
Degradation analysis in a panel of other human cancer cell lines (EOL-1, A-204) confirms the potency of VZ185 (DC 50 between 2 and 8 nM for BRD9). In vitro PK data further showed high stabilities of VZ185 in both plasma and microsomes from both human and mouse species, as well as high aqueous kinetic solubility (up to ~100 μM).