Borussertib

Cas No.:	1800070-77-2
Chemical Name:	N-(2-oxo-3-(1-(4-(5-oxo-3-phenyl-5,6-dihydro-1,6-naphthyridin-2-yl)benzyl)piperidin-4-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)acrylamide
Synonyms:	Borussertib|
SMILES:	C=CC(=O)NC1=CC2=C(C=C1)NC(=O)N2C3CCN(CC3)CC4=CC=C(C=C4)C5=C(C=C6C(=N5)C=CNC6=O)C7=CC=CC=C7
Formula:	C36H32N6O3
M.Wt:	596.691
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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.