keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Poziotinib (NOV120101) 是一种不可逆的 HER1/2/4 抑制剂 (IC50s: 3/5/23 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 352 | 现货 | ||
2 mg | ¥ 503 | 现货 | ||
5 mg | ¥ 907 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,260 | 现货 | ||
50 mg | ¥ 3,360 | 现货 | ||
100 mg | ¥ 4,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 907 | 现货 |
产品描述 | Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). |
靶点活性 | HER1:3 nM, HER2:5 nM, HER4:23 nM |
体外活性 | 在负荷N87人胃癌异种移植物的裸鼠体内,Poziotinib(0.5 mg/kg,p.o.)可明显抑制肿瘤生长,Poziotinib 与 5-FU联用可更有效地抑制肿瘤生长. |
体内活性 | Poziotinib对EGFR磷酸化和下游信号级联放大的关键组分有抑制作用,如STAT3,AKT和ERK,且对HER2扩增的胃癌细胞生长有特异性抑制效果。经激活HER2扩增的胃癌细胞中线粒体途径,Poziotinib还可诱导G1细胞周期阻滞和细胞凋亡。此外,在HER2诱发的和HER2非扩增的胃癌细胞中,Poziotinib与化疗剂有协同效果。 |
激酶实验 | Enzyme activity assay: To determine the IC50 values of HM781-36B for kinase inhibition, enzymes of EGFR, HER2, and HER4 are expressed as recombinant proteins in Sf9 insect cells. Enzyme selectivity screening is then performed using a tyrosine kinase assay kit. Briefly, the reactions are performed in 96 well polystyrene round-bottomed plates containing kinase buffer composed of 100 mM HEPES (pH 7.4), 25 mM MgCl2, 10 mM MnCl2 and 250 μM Na3VO4. The reactions are initiated by the addition of 100 ng/assay enzyme, 100 μM ATP, and 10 ng/mL poly(Glu, Tyr). After 1 h of incubation at room temperature, the reactions are terminated by adding 6 mM EDTA solution and then anti-phosphotyrosine antibody, PTK Green Tracer, and FP dilution buffer mixtures. The fluorescence polarization values are then measured after 30 min at room temperature using a Victor3 microplate reader. Finally, the IC50 values were calculated using the following equation: Y = bottom + (top–bottom)/(1 + 10(X-logIC50)). |
细胞实验 | Viable cell growth is determined by an MTT reduction assay. Briefly, all cell lines are seeded at a density of 3 × 103 per well in 96-well culture plates and then incubated at 37 °C for 24 h. The cells are then treated with 0.001, 0.01, 0.1, or 10 μM of HM781-36B. Three days later, 50 μg of MTT are added to each well and the samples are then incubated for 4 h to reduce the dye. Next, the samples are treated with DMSO, after which the absorbance of the converted dye in the living cells is measured at a wavelength of 540 nm. Six replicate wells are used for each analysis, and at least three independent experiments are conducted. Data points shown represent the mean while bars represent the SE.(Only for Reference) |
别名 | HM781-36B, NOV120101 |
分子量 | 491.34 |
分子式 | C23H21Cl2FN4O3 |
CAS No. | 1092364-38-9 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 91 mg/mL (185.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0353 mL | 10.1763 mL | 20.3525 mL | 50.8813 mL |
5 mM | 0.4071 mL | 2.0353 mL | 4.0705 mL | 10.1763 mL | |
10 mM | 0.2035 mL | 1.0176 mL | 2.0353 mL | 5.0881 mL | |
20 mM | 0.1018 mL | 0.5088 mL | 1.0176 mL | 2.5441 mL | |
50 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0176 mL | |
100 mM | 0.0204 mL | 0.1018 mL | 0.2035 mL | 0.5088 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。
Poziotinib 1092364-38-9 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors HER EGFR NOV-120101 HM781-36B NOV120101 NOV 120101 Inhibitor inhibitor inhibit