BDA-366
BDA-366 is a BCL2-BH4 antagonist. BDA-366 suppresses human myeloma growth. BDA-366 induces robust apoptosis in MM cell lines and primary MM cells by inducing BCL2 conformational change. Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγnull mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. Thus, BDA-366 functions as a novel BH4-based BCL2 inhibitor and offers an entirely new tool for MM therapy.
1: Deng J, Park D, Wang M, Nooka A, Deng Q, Matulis S, Kaufman J, Lonial S, Boise LH, Galipeau J, Deng X. BCL2-BH4 antagonist BDA-366 suppresses human myeloma growth. Oncotarget. 2016 May 10;7(19):27753-63. doi: 10.18632/oncotarget.8513. PubMed PMID: 27049723; PubMed Central PMCID: PMC5053685.
2: Han B, Park D, Li R, Xie M, Owonikoko TK, Zhang G, Sica GL, Ding C, Zhou J, Magis AT, Chen ZG, Shin DM, Ramalingam SS, Khuri FR, Curran WJ, Deng X. Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy. Cancer Cell. 2015 Jun 8;27(6):852-63. doi: 10.1016/j.ccell.2015.04.010. PubMed PMID: 26004684; PubMed Central PMCID: PMC4470473.
3: Vervloessem T, La Rovere R, Bultynck G. Antagonizing Bcl-2's BH4 domain in cancer. Aging (Albany NY). 2015 Oct;7(10):748-9. PubMed PMID: 26525307; PubMed Central PMCID: PMC4637201.
4: Liu Z, Wild C, Ding Y, Ye N, Chen H, Wold EA, Zhou J. BH4 domain of Bcl-2 as a novel target for cancer therapy. Drug Discov Today. 2016 Jun;21(6):989-96. doi: 10.1016/j.drudis.2015.11.008. Review. PubMed PMID: 26631752; PubMed Central PMCID: PMC4882289.
5: Selective Inhibition of BCL2 Shows Antitumor Effects in Lung Cancer. Cancer Discov. 2015 Jul;5(7):OF21. doi: 10.1158/2159-8290.CD-RW2015-102. PubMed PMID: 26045015.
2: Han B, Park D, Li R, Xie M, Owonikoko TK, Zhang G, Sica GL, Ding C, Zhou J, Magis AT, Chen ZG, Shin DM, Ramalingam SS, Khuri FR, Curran WJ, Deng X. Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy. Cancer Cell. 2015 Jun 8;27(6):852-63. doi: 10.1016/j.ccell.2015.04.010. PubMed PMID: 26004684; PubMed Central PMCID: PMC4470473.
3: Vervloessem T, La Rovere R, Bultynck G. Antagonizing Bcl-2's BH4 domain in cancer. Aging (Albany NY). 2015 Oct;7(10):748-9. PubMed PMID: 26525307; PubMed Central PMCID: PMC4637201.
4: Liu Z, Wild C, Ding Y, Ye N, Chen H, Wold EA, Zhou J. BH4 domain of Bcl-2 as a novel target for cancer therapy. Drug Discov Today. 2016 Jun;21(6):989-96. doi: 10.1016/j.drudis.2015.11.008. Review. PubMed PMID: 26631752; PubMed Central PMCID: PMC4882289.
5: Selective Inhibition of BCL2 Shows Antitumor Effects in Lung Cancer. Cancer Discov. 2015 Jul;5(7):OF21. doi: 10.1158/2159-8290.CD-RW2015-102. PubMed PMID: 26045015.
| Chemical | |
|---|---|
| CAS Num | 1821496-27-8 |
| Chemical Formula | C24H29N3O4 |
| Molecular Weight | 423.513 |
| IUPAC Chemical Name | 1-(((S)-3-(diethylamino)-2-hydroxypropyl)amino)-4-((((S)-oxiran-2-yl)methyl)amino)anthracene-9,10-dione |
| Exact Mass | 423.2158 |
| Elemental Analysis | C, 68.06; H, 6.90; N, 9.92; O, 15.11 |
| Synonym | BDA-366; BDA 366; BDA366. |
| Solubility | Soluble in DMSO |
| SMILES Code | CCN(CC)C[C@@H](O)CNC1=CC=C(NC[C@@H]2OC2)C3=C1C(C4=C(C3=O)C=CC=C4)=O |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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