资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-12-14 18:24:50
【药品简介】 伊马替尼(格列卫,Imatinib),酪氨酸激酶抑制剂,是一种小分子蛋白激酶抑制剂,它具有阻断一种或多种蛋白激酶的作用。
【适应症状】 伊马替尼,处方药。用于治疗费城染色体阳性的慢性髓性白血病(Ph+CML)的慢性期、加速期或急变期;用于治疗难治复发成人费城染色体阳性的急性淋巴细胞白血病(Ph+ALL);不能手术切除和/或发生转移的恶性胃肠道间质肿瘤(GIST)的成人患者。
【 药品别名 】 格列卫 甲磺酸伊马替尼 Imatinib
印度伊马替尼(格列卫 甲磺酸伊马替尼 Imatinib)价格,正品图片,治疗白血病药物, 购买伊马替尼请到印度药房官方网站进行购买 【印度药房大全目录】
播放/暂停
生物活性
产品描述 |
matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM). |
靶点活性 |
c-Kit,100 nM (cell free) PDGFR,100 nM (cell free) v-Abl,600nM |
体外活性 |
Imatinib (STI 571) inhibited c-kit autophosphorylation, activation of mitogen-activated protein (MAP) kinase, and activation of Akt without altering total protein levels of c-kit, MAP kinase, or Akt. The concentration that produced 50% inhibition for these effects was approximately 100 nmol/L. STI 571 also significantly decreased SLF-dependent growth of M-07e cells in a dose-dependent manner and blocked the antiapoptotic activity of SLF [1]. Imatinib mesylate had a more similar effect on Bcr/Abl- and c-Kit–dependent proliferation, with an IC50 of 19 nM in R10(-) cells and 82 nM in MO7e cells growing in the presence of SCF (KL, Kit ligand), respectively [2]. STI571 inhibited tyrosine phosphorylation and cell growth of Ba/F3 cells expressing BCR/ABL, TEL/ABL, TEL/PDGFbetaR, and TEL/ARG with an IC(50) of approximately 0.5 microM in each case, but it had no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by TEL/JAK2 [3]. |
体内活性 |
Imatinib (25 mg/kg/day, p.o.) significantly reduced the endometriosis score compared to normal saline. It significantly decreased the ovarian follicle number compared to normal saline. The CD117 staining score of rats administered imatinib was significantly lower than that of the rats received normal saline [4]. After intraperitoneal injection of STI571, it has 80%, 40% and 78% growth inhibition of SCLC6, SCLC61, and SCLC108 tumors, respectively, without any significant inhibition of SCLC74 tumor growth [5]. |
激酶实验 |
PDGF receptor kinase activity: PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels. |
细胞实验 |
M-07e cells were grown in serum-free RPMI 1640 at 37°C for approximately 18 hours before they were incubated for 90 minutes in the presence of various concentrations of STI 571. The cells were then pelleted and resuspended in 1 mL RPMI 1640. STI 571 was added to each tube to achieve the same concentration used during the 90 minutes of preincubation. The cells were then incubated with inhibitor and growth factor (SLF or GM-CSF) for 15 minutes at 37°C. Subsequently, the cell pellets were lysed with 100 to 250 μL of protein lysis buffer (50 mmol/L Tris, 150 mmol/L sodium chloride, 1% NP-40, and 0.25% deoxycholate, with addition of the inhibitors aprotinin, leupeptin, pepstatin, phenylmethyl sulfonyl fluoride, and sodium orthovanadate). Western immunoblot analysis was performed as previously described.41Experiments with HMC-1 cells were performed in the same way except that neither SLF nor GM-CSF was added [1]. 细胞系: BON-1 cells and NCI-H727 cells |
动物实验 |
Swiss mice (nu/nu, female), weighing 30 g, 6 – 8 weeks old, were bred in the animal facilities, maintained under specific pathogen-free conditions with artificial lighting (12 hr light/12 hr dark cycle) and fed a regular diet and water ad libitum. For therapeutic trials, the tumor-bearing mice were randomly divided into equivalent groups of 5 to 12 animals and mice were treated as soon as the xenografted tumors reached a diameter of 5 mm (or a tumor volume of approximately 60 mm^3). Four different human tumors were used: the SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers. STI571 was administered at a total dosage of 70 or 100 mg/kg per day in 1 or 2 intraperitoneal injections, with or without etoposide plus ifosfamide or topotecan. STI571 was diluted in 150 l of H2O and administered on different days, as indicated. Etoposide and ifosfamide were diluted in 200 l of 0.9% sodium chloride, and topotecan was diluted in 150 l of 0.9% sodium chloride. The control group received injections according to the same schedule as experimentally treated mice. All mice were weighed once weekly. Tumor growth was monitored by measuring 2 perpendicular diameters with calipers. Tumor volume (V) and the relative tumor volume (RTV) were calculated as: V = a^2 × b/2, where a is the width (large diameter) and b the length (small diameter) of the tumor in millimeters, and RTV = Vx/Vi, where Vx is the mean tumor volume in cubic millimeters at any given time and Vi is the mean initial tumor volume in cubic millimeters at the start of treatment. Mice were ethically sacrificed when the tumor volume reached 2,500 mm^3 [5]. 动物模型:SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female). |
化学信息
分子量 |
493.60 |
分子式 |
C29H31N7O |
CAS |
152459-95-5 |
溶解度 |
DMSO: 66.9 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 | 2.026 ml | 10.13 ml | 20.259 ml |
5 mM | 0.405 ml | 2.026 ml | 4.052 ml |
10 mM | 0.203 ml | 1.013 ml | 2.026 ml |
50 mM | 0.041 ml | 0.203 ml | 0.405 ml |
伊马替尼对慢性白血病和胃肠道间质瘤疗效非常好,它能为大多数可以负担该药物且能够遵守治疗,并且得到最佳治疗的慢性里细胞...
第一代酪氨酸激酶抑制剂伊马替尼对CML的治疗具有重要价值,而干扰素α是TKI药物诞生前CML治疗的一线药物...
达沙替尼用于治疗成人甲磺酸伊马替尼耐药或不耐受费城染色体阳性(P H)慢性髓系白血病(CML)慢性、加速和急性变性(急性和急...
伊马替尼问世以来,许多慢性粒细胞性白血病患者接受了伊马替尼治疗,但在用药过程中出现了不同程度的不良反应,有时甚至需要...
伊马替尼是治疗慢性粒细胞白血病的有效药物,但需要长期使用。许多慢性粒细胞白血病患者担心长期服用伊马替尼,会给身体带来...
伊马替尼的临床上的常用药物,主要用于白血病的治疗,那么伊马替尼的效果怎么样?用法用量是多少呢?有哪些是需要注意的?...
伊马替尼是国际上公认代替干扰素治疗CML-CP(慢性期)的一线治疗方案,让CML的治疗进入了分子靶向治疗的时代。慢性粒细胞白血病...
伊马替尼是一种常用于治疗白血病的药物。因为很多人对它并不真正了解或害怕它的“副作用”,所以对它有一些怀疑和误解。...
白血病是一种血液病,也称为血癌,治疗非常困难。骨髓移植是一种方法,但患者往往选择其他治疗方法,因为他们找不到合适的骨...
伊马替尼片剂是一种不会经常碰触的药物,因为它是白血病和骨髓发育不良的药物。但是,有些患者对这个药品还是有些疑惑。...
丙肝治疗的药物,干扰素是通过它有一个免疫调节的作用来治疗丙肝...
吉三代的副作用:会有轻微的副作用,类似感冒的症状...
没法来说甲肝、乙肝、丙肝哪一个严重,因为还要根据发病的具体的情况来定...
北京华大中医医院讲解:丙肝患者怎么做才能生育健康宝宝。...
Pharmacy Catalogue
https://www.medicinecenter.org
【价格低廉】【有实体店】【在线客服】 【印度直邮】【有中文网站】【支持银联支付】
Medicine Centre药房成立于1991年, 主要从事批发贸易和出口各种药物注射剂,药物胶囊和药物片剂。该药房的销售网...
www .medplusindia .com
【禁止中国访问】【印度连锁】【品牌实力】
MedPlus是印度第二大药房连锁店。它经营1555家商店,其中1317家为公司所有,159家为特许经营公司,43家为医院药房...
http://www.wellnessforever.in 【药品种类丰富】【渠道正规】【价格较高】
Wellness Forever是一家生活方式零售药房连锁店,致力于为印度本土客户提供全面的健康服务。目前总收入约为620多...
http://www.netmeds.com
【visa/万事达】 【全球可邮】【纯线上销售】【可开处方】
Netmeds.com致力于开发印度本土市场,已成为印度领先的在线药店。Netmeds.com通过其全天候在线门户和移动应用程序...
Buy Drug Pharmacy™是一家零售药品连锁店,通过提供增值服务(如处方管理、船上药剂师处方的数字化、存储健康历...