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BCI-215

BCI-215

产品编号 T7323   CAS 1245792-67-9

BCI-215 是高效肿瘤细胞选择性的双重特异性磷酸酶DUSP-MKP 抑制剂。它对肿瘤细胞有细胞毒性,但对正常细胞无毒性。

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BCI-215 Chemical Structure
BCI-215, CAS 1245792-67-9
规格 价格/CNY 货期 数量
1 mg ¥ 453 现货
2 mg ¥ 656 现货
5 mg ¥ 937 现货
10 mg ¥ 1,530 现货
25 mg ¥ 2,720 现货
50 mg ¥ 3,970 现货
100 mg ¥ 5,780 现货
1 mL * 10 mM (in DMSO) ¥ 995 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: BCI-215 (T7323)
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纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BCI-215 causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling
体外活性 In MDA-MB-231 human breast cancer cells, BCI-215 inhibited cell motility, caused apoptosis but not primary necrosis, and sensitized cells to lymphokine-activated killer cell activity. Mechanistically, BCI-215 induced rapid and sustained phosphorylation of extracellular signal-regulated kinase (ERK), p38, and c-Jun N-terminal kinase (JNK) in the absence of reactive oxygen species, and its toxicity was partially rescued by inhibition of p38 but not JNK or ERK. BCI-215 also hyperactivated MKK4/SEK1, suggesting activation of stress responses[1].
细胞实验 Peripheral blood mononuclear cells were obtained from healthy volunteers. Cells were cultured in RPMI 1640 supplemented with 10% fetal calf serum, 1% glutamine, and 1% penicillin/streptomycin, and stimulated with 6,000 IU of Interleukin 2 for 24 hours. After incubation, cells were washed with PBS and counted. In parallel, MDA-MB-231 cells were pretreated in a 384-well plate with vehicle or BCI-215 (3 μM). After 24 hours in culture, medium was replaced and peripheral blood mononuclear cells (PBMCs) added in 2-fold serial dilutions starting with a 50-fold excess of PBMCs in triplicate. After 24 hours of coculture, cells were fixed with formaldehyde/Hoechst 33342, washed twice with PBS, and imaged on the ArrayScan II. Cancer cells were identified by their larger nuclei compared with PBMCs, setting a size gate in the Hoechst channel. In experiments with chemotherapeutics, cells carrying a biosensor consisting of a mitochondrial targeting sequence derived from cytochrome c oxidase VIII linked to GFP that is a surrogate for cytochrome c release from mitochondria were pretreated for 24 hours with cisplatin (2 μM) or doxorubicin (400 nM), exposed to LAK, and cancer cells were identified and quantified by green fluorescence. Cell densities were normalized to those in the absence of PBMCs. Mean cell densities from multiple independent experiments were averaged and plotted in GraphPad Prism version 7.00[1].
分子量 396.32
分子式 C22H22BrNO
CAS No. 1245792-67-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 3.96 mg/mL (10 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5232 mL 12.6161 mL 25.2321 mL 63.0803 mL
5 mM 0.5046 mL 2.5232 mL 5.0464 mL 12.6161 mL
10 mM 0.2523 mL 1.2616 mL 2.5232 mL 6.308 mL

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TargetMol Library Books参考文献

2. Kaltenmeier C T , Vollmer L L , Vernetti L A , et al. A Tumor Cell-Selective Inhibitor of Mitogen-Activated Protein Kinase Phosphatases Sensitizes Breast Cancer Cells to Lymphokine-Activated Killer Cell Activity[J]. Journal of Pharmacology and Experimental Therapeutics, 2017, 361(1):39-50.
DT-061 Eurestobart AS1949490 Auten-99 HBr Sodium stibogluconate Bis(maltolato)oxovanadium(IV) PTP1B-IN-3 PTP1B-IN-1

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌活性化合物库 已知活性化合物库 经典已知活性库 糖代谢化合物库 抗癌化合物库 代谢化合物库 NO PAINS 化合物库 磷酸酶抑制剂化合物库

TargetMol Calculator剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

TargetMol Calculator 体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
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给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

BCI-215 1245792-67-9 Metabolism Phosphatase specificity BCI 215 DUSP-MKP inhibit Inhibitor MAPK BCI215 dual inhibitor

 

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