资料发布时间:2018-10-30 14:50:00 最后更新时间: 2021-06-09 15:17:08
【药品简介】 厄洛替尼可试用于两个或两个以上化疗方案失败的局部晚期或转移的非小细胞肺癌的三线治疗。
【适应症状】 厄洛替尼,处方药。非小细胞肺癌: 有表皮生长因子受体EGFR 19号外显子缺失或21号外显子(L858R)突变的转移性非小细胞肺癌的一线用药;或晚期非小细胞肺癌首次化疗无效后;或作为晚期非小细胞肺癌稳定期的维持用药(4个疗程的含铂化疗方案后)。胰腺癌:与吉西他滨联用,作为局部晚期或无法切除或转移性胰腺癌的一线用药。
【 药品别名 】 特罗凯 厄洛替尼 Tarcevav Erlotinib Hydrochloride Tablets
印度厄洛替尼(特罗凯 厄洛替尼 Tarcevav Erlotinib Hydrochloride Tablets)价格,正品图片,治疗胰腺癌药物, 购买厄洛替尼请到印度药房官方网站进行购买 【印度药房大全目录】
【 市场参考价格 】 ¥480.00~950.00
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生物活性
产品描述 |
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer. |
靶点活性 |
EGFR/HER1,2nM |
实验溶液 |
15% Captisol: 16 mg/mL warmed |
体外活性 |
Erlotinib(10 uM)抑制EGFR在Y1068(自磷酸化) 和Y845 (Src依赖性磷酸化) 位点磷酸化。Erlotinib不影响SBC-5细胞增殖,但是以剂量依赖的方式明显抑制PC-9细胞(在EGFR基因第19外显子含缺失突变)增殖。Erlotinib对SBC-5细胞迁移也没有作用。Erlotinib抑制Capan-1细胞和HPAC细胞生长, IC50 分别为3和1.1μM。Erlotinib作用于HNS人颈部和头部肿瘤细胞,能明显抑制EGFR自磷酸化,上述肿瘤细胞是EGFR高表达的细胞系。只有作用于最敏感的细胞株时,Erlotinib才能抑制细胞外信号调节激酶Akt和S6。 |
体内活性 |
单独作用于H460a肿瘤模型时,Erlotinib以剂量依赖性方式抑制肿瘤生长,且与药物循环水平相关。 |
激酶实验 |
Kinase assays: 96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes. |
细胞实验 |
Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software.(Only for Reference) 细胞系: A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells |
动物实验 |
动物模型:5-week-old BALB-nu/nu with HPAC cells |
化学信息
分子量 |
429.90 |
分子式 |
C22H23N3O4·HCl |
CAS |
183319-69-9 |
溶解度 |
DMSO: 9.3 mM ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 2.326 ml | 11.631 ml | 23.261 ml |
5 mM | 0.465 ml | 2.326 ml | 4.652 ml |
10 mM | 0.233 ml | 1.163 ml | 2.326 ml |
50 mM | 0.047 ml | 0.233 ml | 0.465 ml |
【药品特色】 在体外和或体内研究中通过依维莫司mTOR的抑制作用显示减低细胞增殖,抑制血管生成和葡萄糖摄取。依维莫司适用......
【作用机制】 通过抑制多个受体酪氨酸激酶,达到抑制肿瘤和新生血管形成的作用。抑制包括血小板分化生长因子(PDGFR-al......
【作用机制】 厄洛替尼是一个酪氨酸激酶抑制剂(TKI),可逆性的抑制特定类型的EGFR突变。EGFR(表皮生长因子受体)......
【给药方法】 每天一次,空腹服用(饭前一小时或饭后2小时) 厄洛替尼单药用于非小细胞肺癌的推荐剂量为150mg/日,至少......
一项Ⅲ期安慰剂对照临床研究的结果表明,厄洛替尼每13名患者口服150毫克单药治疗可显著延长晚期复发性非小细胞肺癌(NSC......
随着对肿瘤分子生物学机制研究的深入,越来越多的肿瘤靶向治疗逐渐发展并应用于临床,取得了良好的治疗效果。厄洛替尼是一种新型......
厄洛替尼作为一种EGFR抑制剂,它具有高效、低毒、副作用小的特点。但是,如果患者在服用过程中饮食不当,也会影响其疗效,并......
与其他靶向抗肿瘤药物一样,厄洛替尼抑制肿瘤细胞生长,促进肿瘤细胞凋亡,同时对人体也有一定的副作用。在这个时候,即使我们不......
厄洛替尼是一种表皮生长因子受体酪氨酸激酶抑制剂,在许多临床试验和具体治疗实例中取得了良好的效果。 2007年3月17日,......
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