BDA-366

製品コードS7849 バッチS784901

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C24H29N3O4

分子量 423.5 CAS No. 1909226-00-1
Solubility (25°C)* 体外 DMSO 84 mg/mL (198.34 mM)
Ethanol 5 mg/mL (11.8 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 BDA-366は、低分子Bcl2-BH4ドメインアンタゴニストであり、BH4に高い親和性と選択性で結合します。
in vitro BDA-366 induces robust apoptosis in MM(Multiple myeloma) cell lines and primary MM cells by inducing BCL2 conformational change. This compound 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. It did not bind to other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1, indicating the specificity of its Bcl2 binding. This chemical 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 null mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. Also, this compound suppresses lung cancer growth via induction of apoptosis in animal models. The BH4 antagonist exhibits potent efficacy against human lung cancer in vivo without platelet reduction.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human MM RPMI8226 and U266 cell lines
濃度 0, 0.1, 0.25, 0.5 μM
反応時間 48 h
実験の流れ Human MM cell lines RPMI8226 and U266 were treated with BDA-366 at increasing concentrations (0, 0.1, 0.25, 0.5μM) for 48hr. Cells were harvested, stained with Annexin V and propidium iodide (PI), and subjected to FACS analysis. Apoptotic cells were gated on the Annexin V positive population. Annexin V+PI− cells were early apoptotic cells, Annexin+PI+ cells were late apoptotic cells, and Annexin−PI+ cells were necrotic cells.
動物実験 動物モデル NSG mice
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27049723/
  • https://pubmed.ncbi.nlm.nih.gov/26004684/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

BDA-366 inhibits extra-nodal natural killer/T-cell lymphoma by inducing mitochondria damage through NF-κB pathway [ Biochem Pharmacol, 2025, S0006-2952(25)00712-9] PubMed: 41135664
CYD0281, a Bcl-2 BH4 domain antagonist, inhibits tumor angiogenesis and breast cancer tumor growth [ BMC Cancer, 2023, 23(1):479] PubMed: 37237269

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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