Information BDA-366 is a small-moleculeBcl2-BH4domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM). Targets Bcl2-BH4 (Cell-free assay) 3.3 nM(Ki) In vitro BDA-366 induces robust apoptosis in MM(Multiple myeloma) cell lines and primary MM cells by inducing BCL2 conformational change. BDA-366 induces a conformational change in the BCL2 molecule that converts it to a death protein, and inhibits lung cancer growth in vitro and in vivo. BDA-366 did not bind to other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1, indicating the specificity of its Bcl2 binding. BDA-366 induces apoptotic cell death in a Bax-dependent manner and induces calcium (Ca2+) release via inhibition of Bcl2/IP3R interaction. In vivo Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγ mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. Also, BDA-366 suppresses lung cancer growth via induction of apoptosis in animal models. The BH4 antagonist BDA-366 exhibits potent efficacy against human lung cancer in vivo without platelet reduction. Cell Research(from reference) Cell lines：human MM RPMI8226 and U266 cell lines Concentrations：0, 0.1, 0.25, 0.5 μM Incubation Time：48 h
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BDA-366
CAS number：1909226-00-1 molecular formula：C24H29N3O4
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| Chinese alias | - | ||
| English alias | 1-[[3-(Diethylamino)-2(S)-hydroxypropyl]amino]-4-[(2(S)-oxiranylmethyl)amino]-9,10-anthracenedione | ||
| CAS number | 1909226-00-1 | molecular formula | C24H29N3O4 |
| molecular weight | 423.5 g/mol | Exact mass | ≥97% |
| PSA | 94.200 Ų | logp | 2.467 |
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