BTSA1

製品コードS8650 バッチS865001

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

C₂₁H₁₄N₆OS₂

分子量

430.51

CAS No.

314761-14-3

Solubility (25°C)*

体外

DMSO

81 mg/mL (188.14 mM)

Water

Insoluble

Ethanol

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。	2.000mg/ml (4.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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。	0.200mg/ml (0.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 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	BTSA1は、N末端活性化部位に高い親和性と特異性で結合し、BAXの立体構造変化を誘導してBAXを介したアポトーシスを促進する、薬理学的に最適化されたBAX活性化因子です。健康な細胞を温存しつつ、白血病細胞株および患者サンプルにおいてアポトーシスを効果的に促進します。
in vitro	BTSA1 has no capacity to directly activate the pro-apoptotic homolog BAK. This compound treatment potently and dose-responsively induces membrane translocation of recombinant soluble BAX to mitochondrial membrane, which is followed by induction of BAX oligomerization. This chemical-induced BAX activation promotes apoptosis in cancer cells. It reduces viability of all AML cell lines in a dose-dependent manner with IC50 values ranged between 1 and 4 μM, which leads to complete effect within 24 hr treatment. It induces dose-dependent caspase-3/7 activation in all five AML cell lines.
in vivo	BTSA1 potently suppresses human acute myeloid leukemia (AML) xenografts and increases host survival without toxicity. It is well-tolerated in mice with no toxic effects on healthy hematopoiesis, including healthy stem cellenriched (LSK) cells, common myeloid progenitors, granulocyte-monocyte progenitors, and megakaryocyte-erythrocyte progenitors. This compound has substantial half-life in mouse plasma (T_1/2 = 15 hr) and oral bioavailability (%F = 51), while a 10 mg/kg dose reaches sufficient levels (~15 μM) of the compound to induce BAX activation and apoptosis in leukemia cells. Thus, it is orally bioavailable with excellent pharmacokinetics, has significant anti-tumor activity in leukemia xenografts by promoting apoptosis, and at therapeutically effective doses it does not show any detectable toxicity in the hematopoietic system or other tissues.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	AML cells
	濃度	--
	反応時間	2.5 hr
	実験の流れ	AML cells (2 × 10⁴ cells/well) are seeded in 96-well white plates and incubated with serial dilutions of BTSA1 or this compound or vehicle (0.15% DMSO) in no FBS media for 2.5 hr, followed by 10% FBS replacement to a final volume of 100 μl. Cell viability is assayed at 24 hr.
動物実験	動物モデル	6-8 weeks old NOD-SCID IL2Rg null (NSG) mice/6-8 weeks old ICR (CD-1) male mice
	投薬量	10 mg/kg
	投与方法	by an oral gavage or intravenous injection

参考

https://pubmed.ncbi.nlm.nih.gov/29017059/

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：

Gravitational and mechanical forces drive mitochondrial translation [ bioRxiv, 2024, 10.1101/2023.01.18.524628]	PubMed: none
Intracellular FGF1 protects cells from apoptosis through direct interaction with p53 [ Cell Mol Life Sci, 2023, 80(10):311]	PubMed: 37783936
Mitochondrial Drp1 recognizes and induces excessive mPTP opening after hypoxia through BAX-PiC and LRRK2-HK2 [ Cell Death Dis, 2021, 12(11):1050]	PubMed: 34741026
FILIP1L-mediated cell apoptosis, epithelial-mesenchymal transition and extracellular matrix synthesis aggravate posterior capsular opacification [ Life Sci, 2021, S0024-3205(21)01048-1]	PubMed: 34666037

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。