Formulation: A solid
Formal Name: 1-[[(2S)-3-(diethylamino)-2-hydroxypropyl]amino]-4-[[(2S)-2-oxiranylmethyl]amino]-9,10-anthracenedione
Purity: ≥98%
Formula Markup: C24H29N3O4
Formula Weight: 423,5
Shelf life (days): 1460
CAS Number: 1909226-00-1
Notes: BDA-366 is an antagonist of the BH4 domain of the anti-apoptotic protein Bcl-2 (Ki = 3.3 nM).{65183} It is selective for Bcl-2 over Bcl-xL, Mcl-1, A1/Bfl-1, and Bcl-2 lacking the BH4 domain (Kis = >500, >500, >500, and 654.8 nM, respectively) but does bind to BH1-, BH2-, or BH3 domain-deficient Bcl-2 (Kis = 12.4, 7.6, and 23.4 nM, respectively). However, BDA-366 (10 µM) induces Bax activation in HT cells, which lack endogenous Bcl-2, and in HT cells overexpressing Bcl-2, indicating a context-specific Bcl-2-independent mechanism of cell death.{65184} BDA-366 is cytotoxic against a panel of non-small cell lung cancer (NSCLC) and SCLC cell lines (IC50s = 0.2-1.73 µM).{65183} It also reduces tumor growth and induces tumoral caspase-3 activation in an H460 lung cancer mouse xenograft model when administered at doses of 10, 20, and 30 mg/kg.{65184}
English
Deutsch
