PROTAC BET degrader-2;4-[(5-cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-[3-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]propyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide;9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]propyl]-6-methoxy-
Cas No.
2093388-33-9
分子式
C41H42N10O6
分子量
770.84
包装储存
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
PROTAC BET degrader-2 是由Cereblon配体和BET配体相连的PROTAC,在 RS4;11 细胞中测得其对细胞生长的 IC50 值为 9.6 nM,并能实现肿瘤消退。
生物活性
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC 50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
性状
Solid
IC50 & Target[1][2]
IC50: 9.6 nM (BET in the RS4;11 leukemia cell line).
体外研究(In Vitro)
PROTAC BET degrader-2 (compound 25) is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
溶解度数据
In Vitro: DMSO : 50 mg/mL (64.86 mM; Need ultrasonic)配制储备液