BDA-366

製品コードS7849 バッチS784902

印刷

化学情報

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

6 mg/mL (14.16 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.200mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 84 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.710mg/ml (1.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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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