Borussertib |
| Catalog No.GC65367 |
Le borussertib est un inhibiteur covalent allostérique et premier de sa classe de la protéine kinase Akt, avec une IC50 de 0,8 nM et un Ki de 2,2 nM pour Aktwt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1800070-77-2
Sample solution is provided at 25 µL, 10mM.
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Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt[1].
Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. 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].
[1]. Niklas Uhlenbrock, et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.
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