bda 366

BDA-366, a potent Bcl2 antagonist, selectively binds the Bcl2-BH4 domain with high affinity (Ki = 3.3 nM), inducing a conformational change that nullifies its antiapoptotic function, thereby transforming it into a pro-apoptotic entity. This compound effectively suppresses lung cancer cell growth[1].

(Rac)-BDA-366 (example 2) is the racemate of BDA-366, a potent Bcl-2 antagonist with a Ki of 3.3 nM. It shows high affinity and selectivity for the Bcl-2-BH4 domain. BDA-366 induces a conformational change in Bcl-2, neutralizing its anti-apoptotic function and converting Bcl-2 from a survival molecule into a cell death inducer. Additionally, BDA-366 can inhibit the growth of lung cancer cells.

CYD-2-88 (BDA-366 analog) is an analog of BDA-366 (Bcl2 BH4 antagonist). Administered through intraperitoneal injection at a dosage of 20 mg kg, CYD-2-88 effectively inhibits tumor growth in mice with NSCLC H460 xenografts.