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BIBF0775

BIBF0775

产品编号 T5197   CAS 334951-90-5

BIBF0775 是一种选择性的TGFβI 型受体抑制剂(IC50:34 nM)。

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BIBF0775 Chemical Structure
BIBF0775, CAS 334951-90-5
规格 价格/CNY 货期 数量
1 mg ¥ 528 现货
5 mg ¥ 1,490 现货
10 mg ¥ 2,320 现货
25 mg ¥ 3,830 现货
50 mg ¥ 5,390 现货
100 mg ¥ 7,380 现货
500 mg ¥ 14,700 现货
1 mL * 10 mM (in DMSO) ¥ 1,630 现货
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
Doxorubicin hydrochloride限时半价
产品目录号及名称: BIBF0775 (T5197)
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纯度: 99.45%
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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 BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
靶点活性 ALK5:34 nM
激酶实验 The inhibition of the kinase activity of TGFβRI was determined using the Promega Kinase-Glo kit according to the manufacturer's protocol in the presence of 600 nM ATP. N-terminally his-tagged human TGFβRI (aa 162-end) expressed in baculovirus and purified using nickel affinity chromatography was used at a final concentration of 0.03 μg/mL. The inhibition of the kinase activity of PDGFRR was determined using the Z0-LYTE assay technology according to the manufacturer's protocol. Full-length human PDGFRR (5.6 nM per assay) and the Tyr4 peptide (2 μM per assay) were obtained from Invitrogen, too. IC50 values were determined by the use of the Graph PadPrism software.
细胞实验 The high-content cytotoxicity assay (kit I) was performed according to the manufacturer's instructions. HaCaT cells were cultured overnight in black 96-well plates, incubated for 24 h with each compound at different concentrations, and stained with cytotoxicity cocktail. Cells were fixed, washed, and scanned on the Cellomics ArrayScan II platform. Images were analyzed with the Cell Health image analysis algorithm. Cytotoxicity indices were calculated for each of the four parameters (cellular membrane integrity, nuclear fragmentation and density, and lysosomal mass) to indicate the percentage of cells outside of the normal range which was defined using a vehicle-treated reference cell population.
分子量 494.63
分子式 C31H34N4O2
CAS No. 334951-90-5

存储

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

溶解度

DMSO: 60 mg/mL

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TargetMol Library Books参考文献

1. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI). J Med Chem. 2010 Oct 28;53(20):7287-95.
LDN193189 GSK1838705A Belizatinib GW788388 AZD-3463 ASP3026 LDN-193189 2HCl LDN-193189 HCl

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 TGF-β/Smad靶点化合物库 激酶抑制剂库 酪氨酸激酶分子库 共价抑制剂库 细胞重编程化合物库 干细胞分化化合物库 抗肺癌化合物库 抗乳腺癌化合物库 抗纤维化化合物库

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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。

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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

BIBF0775 334951-90-5 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad BIBF-0775 inhibit Transforming growth factor beta receptors TGF-β Receptor BIBF 0775 Inhibitor inhibitor

 

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