Poziotinib
作者：齊岳
發(fā)布時(shí)間：2023-08-30
09:02:40
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Poziotinib
產(chǎn)品描述：
| 產(chǎn)品描述 | Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). |
| 靶點(diǎn)活性 | HER4:23 nM, HER2:5 nM, HER1:3 nM |
| 體外活性 | 在負(fù)荷N87人胃癌異種移植物的裸鼠體內(nèi),Poziotinib（0.5 mg/kg,p.o.）可明顯抑制腫瘤生長(zhǎng),Poziotinib 與 5-FU聯(lián)用可更有效地抑制腫瘤生長(zhǎng). |
| 體內(nèi)活性 | Poziotinib對(duì)EGFR磷酸化和下游信號(hào)級(jí)聯(lián)放大的關(guān)鍵組分有抑制作用,如STAT3,AKT和ERK,且對(duì)HER2擴(kuò)增的胃癌細(xì)胞生長(zhǎng)有特異性抑制效果。經(jīng)激活HER2擴(kuò)增的胃癌細(xì)胞中線粒體途徑,Poziotinib還可誘導(dǎo)G1細(xì)胞周期阻滯和細(xì)胞凋亡。此外,在HER2誘發(fā)的和HER2非擴(kuò)增的胃癌細(xì)胞中,Poziotinib與化療劑有協(xié)同效果。 |
| 激酶實(shí)驗(yàn) | 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)). |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 別名 | HM781-36B, NOV120101 |
| 分子量 | 491.34 |
| 分子式 | C23H21Cl2FN4O3 |
| CAS No. | 1092364-38-9 |
存儲(chǔ)
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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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