Borussertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Borassertib 是一种有效的、一流的共价变构 AKT 抑制剂。

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.

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Borussertib

Cytoskeleton/Cell Adhesion Molecules

Akt

Akt

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1800070-77-2

596.691

C36H32N6O3

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (41.90 mM)

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