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BDA-366 is an antagonist of the BH4 domain of the anti-apoptotic protein Bcl-2 (Ki = 3.3 nM). 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. BDA-366 is cytotoxic against a panel of non-small cell lung cancer (NSCLC) and SCLC cell lines (IC50s = 0.2-1.73 µM). 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.Formal Name: 1-[[(2S)-3-(diethylamino)-2-hydroxypropyl]amino]-4-[[(2S)-2-oxiranylmethyl]amino]-9,10-anthracenedione. CAS Number: 1909226-00-1. Molecular Formula: C24H29N3O4. Formula Weight: 423.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 2 mg/ml. lambdamax: 255, 590, 635 nm. SMILES: CCN(CC)C[C@@H](O)CNC(C=C1)=C(C(C2=CC=CC=C2C3=O)=O)C3=C1NC[C@H]4CO4. InChi Code: InChI=1S/C24H29N3O4/c1-3-27(4-2)13-15(28)11-25-19-9-10-20(26-12-16-14-31-16)22-21(19)23(29)17-7-5-6-8-18(17)24(22)30/h5-10,15-16,25-26,28H,3-4,11-14H2,1-2H3/t15-,16-/m0/s1. InChi Key: JYOOEVFJWLBLKF-HOTGVXAUSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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