Borussertib

Research use only, not for human use.

Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor.

Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor; specifically binds to two non-catalytic cysteines in AKT at 120 positions 296 and 310; exhibits pronounced sensitivity to breast cancer cell line ZR-75-1 with EC50 of 5 nM, 7- to 12-fold higher potency compared to reversible allosteric inhibitor miransertib and MK-2206; demonstrated strong antiproliferative activity in cancer cell lines harboring genetic alterations within the PTEN, PI3K, and RAS signaling pathways,b displayed antitumor activity in combination with the MEK inhibitor trametinib in patient-derived xenograft models of mutant KRAS pancreatic and colon cancer.

Borussertib

Cytoskeleton/Cell Adhesion Molecules

Akt

Akt

——

——

1800070-77-2

596.69

C36H32N6O3

>98% (HPLC)

——

C=CC(NC1=CC=C(C(N2C3CCN(CC4=CC=C(C5=NC6=C(C(NC=C6)=O)C=C5C7=CC=CC=C7)C=C4)CC3)=C1)NC2=O)=O

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

(-20℃)

With Ice Pack

≥ 2 years