Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BTSA1 是一种有口服活性的 BAX 激活剂,IC50为 250 nM,EC50为 144 nM。它以高亲和力和特异性与 N 末端激活位点结合,并诱导 BAX 发生构象变化,从而导致BAX 介导的细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | BTSA1 is a BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. |
靶点活性 | Bax:250 nM (IC50), Bax:144 nM (EC50) |
体外活性 | BTSA1 has no capacity to directly activate the pro-apoptotic homolog BAK. BTSA1 treatment potently and dose-responsively induces membrane translocation of recombinant soluble BAX to the mitochondrial membrane, which is followed by induction of BAX oligomerization. BTSA1-induced BAX activation promotes apoptosis in cancer cells. BTSA1 reduces the 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[1]. |
体内活性 | 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 cell-enriched (LSK) cells, common myeloid progenitors, granulocyte-monocyte progenitors, and megakaryocyte-erythrocyte progenitors. BTSA1 has a substantial half-life in mouse plasma (T1/2 = 15 hr) and oral bioavailability (%F = 51), while a 10 mg/kg dose reaches sufficient levels (~15 μM) of BTSA1 to induce BAX activation and apoptosis in leukemia cells. Thus, BTSA1 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[1]. |
分子量 | 430.51 |
分子式 | C21H14N6OS2 |
CAS No. | 314761-14-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (139.37 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3228 mL | 11.6141 mL | 23.2283 mL | 58.0707 mL |
5 mM | 0.4646 mL | 2.3228 mL | 4.6457 mL | 11.6141 mL | |
10 mM | 0.2323 mL | 1.1614 mL | 2.3228 mL | 5.8071 mL | |
20 mM | 0.1161 mL | 0.5807 mL | 1.1614 mL | 2.9035 mL | |
50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1614 mL | |
100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.5807 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BTSA1 314761-14-3 Apoptosis BCL inhibit FITC-BIM caspase-3/7 translocation BTSA 1 Bcl-2 Family BTSA-1 viability Inhibitor mitochondrial pharmacologically BAX AML SAHBA2 inhibitor