Borussertib

Names

[ Name ]:
Borussertib

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

Aktwt:0.8 nM (IC50)

Aktwt:2.2 nM (Ki)

[In Vitro]

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].

[References]

[1]. Niklas Uhlenbrock, et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₆H₃₂N₆O₃

[ Molecular Weight ]:
596.68

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.