Poziotinib
作者：齐岳
发布时间：2023-08-30
09:02:40
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产品名称：Poziotinib
产品描述：
| 产品描述 | Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). |
| 靶点活性 | HER4:23 nM, HER2:5 nM, HER1:3 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 |
存储
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 91 mg/mL (185.2 mM)
H2O: <1 mg/mL
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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