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】 2014年1月10日美国食品药品监督管理局(FDA)批准曲美替尼与达拉非尼联用治疗有不可切除的(不能外科手术)和转移晚期黑色素瘤患者。达拉非尼不适用于野生型BRAF-患者的治疗。
【适应症状】 达拉非尼,1) 达拉非尼是一种激酶抑制剂,达拉非尼适用于有不能切除或转移黑色素瘤; 2) 达拉非尼与曲美替尼联用是适用于被FDA批准检验检出BRAF V600E或V600K突变有不可切除的或转移黑色素瘤患者的治疗。
【 药品别名 】 达拉非尼 Dabrafenib TAFINLAR
印度达拉非尼(达拉非尼 Dabrafenib TAFINLAR)价格,正品图片,治疗黑色素瘤药物, 购买达拉非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 】 ¥11000.00~15300.00
播放/暂停
生物活性
产品描述 |
Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf). |
靶点活性 |
B-Raf,3.2nM B-Raf (V600E),0.8nM C-Raf,5.0nM |
实验溶液 |
30% PEG400+0.5% Tween80+5% propylene glycol: 8 mg/mL |
体外活性 |
Dabrafenib (GSK2118436) was a potent biochemical inhibitor of B-RafV600E, wild-type B-Raf, and c-Raf. GSK2118436 was significantly less effective at inhibiting SMAD2/3 phosphorylation (IC50: 3.7 μM) compared with inhibiting ERK phosphorylation (IC50: 4 nM) in a cellular context [1]. Dabrafenib inhibited the release of HMGB1 and downregulated HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells [2]. Stable knockdown of NRAS with short hairpin RNA partially restored GSK2118436 sensitivity in mutant NRAS clones, whereas expression of NRAS(Q61K) or NRAS(A146T) in the A375 parental cells decreased sensitivity to GSK2118436. Expression of MEK1(K59del), but not MEK1(P387S), decreased the sensitivity of A375 cells to GSK2118436 [3]. |
体内活性 |
GSK2118436 dramatically reduced tumor growth in mice bearing B-RafV600E human melanoma tumors. In this model, CD1 nu/nu mice bearing A375P F11 (B-RafV600E) tumors were dosed orally with GSK2118436 at doses of 0.1, 1, 10, and 100 mg/kg once daily for 14 days. Dose-proportional reductions in tumor growth were observed. In the 100 mg/kg group, complete tumor regression was observed in 50% of treated animals [1]. The vaginal opening (VO) occurred earlier in Dabrafenib (DAB) females than in controls; however, the timing of the first estrus was unaffected. DAB-treated females evaluated just before VO had mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females had keratinized and histologically open vaginas [4]. |
细胞实验 |
For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner. |
动物实验 |
动物模型:rats |
化学信息
分子量 |
519.56 |
分子式 |
C23H20F3N5O2S2 |
CAS |
1195765-45-7 |
溶解度 |
DMSO: 28 mg/mL (53.9 mM) Ethanol: <1 mg/mL ( < 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 | 1.925 ml | 9.624 ml | 19.247 ml |
5 mM | 0.385 ml | 1.925 ml | 3.849 ml |
10 mM | 0.192 ml | 0.962 ml | 1.925 ml |
50 mM | 0.038 ml | 0.192 ml | 0.385 ml |
有很多患者再问,印度达拉非尼的疗效怎么样?癌症是一种多见的症状,严重影响着大家的身体健康。在这个谈癌色变的年代,寻找到其......
虽然黑色素瘤的发病率没有肺癌和肝癌高,但不能手术的晚期患者死亡率相对较高,因此对该病的治疗不可低估。达拉非尼常与曲美替尼......
在一项关于达拉非尼/曲美替尼治疗黑色素瘤的临床研究中,证明了达拉非尼/曲美替尼与黑色素瘤生存期之间的关系。依照该阶段研究......
黑色素瘤本身是一种非常危险的肿瘤。如果你想最大限度地提高患者的生存率,唯一能做的就是尽快做出诊断。我国皮肤恶性肿瘤的发病......
黑色素瘤协会(SMR),达拉非尼 + 曲美替尼(dabrafenib + trametinib)...
黑色素瘤又称恶性黑色素瘤多见于30岁以上的成年人,多发于皮肤以足底、外阴、肛门周围。...
根据病灶的浸润深度、有没有溃疡或者淋巴结转移的情况等,这些危险因素一般将术后的患者分为四类...
靶向治疗是一种只针对肿瘤细胞的治疗,不良反应小。...
Pharmacy Catalogue
【代购】【有实体店】【在线客服懂中文】
代购+直邮,印度抗癌药跨境医药电商直邮服务,让肿瘤患者能够有更好的选择,平台提供印度就医,印度易瑞沙,吉三代,吉二代,索......
【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......
【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62......
【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......