Borussertib 是一种蛋白激酶Akt的共价变构抑制剂,其对 Aktwt的IC50=0.8 nM,Ki=2.2 nM。
产品描述
Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt(IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt)
体外活性
Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. With the EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively[1].
Cas No.
1800070-77-2
分子式
C36H32N6O3
分子量
596.68
储存和溶解度
DMSO:25 mg/mL (41.90 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years