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AP26113說明書-靶向藥AP26113原料藥哪里有賣渠道

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品牌: XXJL
含量: 99%
起訂: 1 克
供貨總量: 1000 克
發貨期限: 自買家付款之日起 3 天內發貨
所在地: 湖北 武漢市
有效期至: 長期有效
最后更新: 2019-06-18 10:04
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【AP26113說明書-靶向藥AP26113原料藥哪里有賣渠道】詳細說明
 *新AP26113原料藥(http://www.agtcmy.tw/sell/17/)現貨購買方式, AP26113原料藥(http://www.agtcmy.tw/sell/17/)購買途徑 AP26113原料藥價格 AP26113原料藥用量 AP26113原料藥副反應 AP26113原料**果
中文名 AP26113 
英文名 AP26113 
別    稱 5-氯-N2-[4-[4-(二甲基氨基)-1-哌啶基]-2-甲氧基苯基]-N4-[2-(二甲基亞膦酰)苯基]-2,4-嘧啶二胺 
化學式 C26H34ClN6O2P 
CAS: 1197958-12-5
含量:99.7%
包裝(http://www.agtcmy.tw/sell/99/):5g、10g
作用:AP26113是一種**的ALK抑制劑,用于ALK突變陽性的非小細胞肺癌。用于克唑替尼耐藥后**。

Detailed Description:

The drug being tested in this study is called Brigatinib (AP26113). Brigatinib is being tested to treat people with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This study will look at the efficacy of Brigatinib.

The study enrolled 222 patients. Participants will be randomly assigned (by chance, like flipping a coin) to one of the two treatment groups:

  • Brigatinib 90 mg
  • Brigatinib 90 mg -180 mg

產品(http://www.agtcmy.tw/invest/)描述

Brigatinib is a excellently effective and specific ALK inhibitor( IC50 =0.6 nM).

靶點活性

ALK,0.07nM

EGFR (C797S/del19),28.4nM

EGFR (del19),36.8nM

IGF-1R,32nM

實驗溶液

NMP+polyethylene glycol 300 (10+90, v+v): 30 mg/mL

體外活性

在SU-DHL-1(GI50=9 nM), H3122 (GI50=4 nM)和 Ba/F3-EML4-ALK v1(1GI50=3 nM)細胞系中,抑制生長細胞生長。在表達EGFR-DEL(HCC827)的NSCLC細胞系中(IC50=62nM),AP26113作用于抑制EGFR 磷酸化,抑制細胞生長。

體內活性

在HCC827(EGFR-DEL)或HCC827(EGFR-DEL/T790M)移植瘤小鼠模型中,AP26113(25 mg/kg),能夠抑制腫瘤細胞生長。在Karpas-299移植瘤小鼠模型中,AP26113(<50 mg/kg)抑制p-ALK。在Karpas-299移植瘤小鼠模型和 H3122 移植瘤小鼠模型中,AP26113(<50 mg/kg)抑制腫瘤生長。

細胞實驗

Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3 nM to 10 μM. After 72 h of drug treatment, cell viability is measured using the CellTiter-Glo assay. (only for Reference)

細胞系: Ba/F3 cells

化學信息

分子量

529.01

分子式

C26H34ClN6O2P

CAS

1197958-12-5

溶解度

DMSO: 42 mg/mL (79.4 mM)

Ethanol: 98 mg/mL (185.3 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

儲存條件

3 years  -20℃  powder

2 years  -80℃  In solvent

備注

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.


All participants will be asked to take tablet, orally once daily until disease progression or intolerable toxicity. Participants in Brigatinib 90 mg - 180 mg received 180 mg with a 7-day lead-in at 90 mg.

This multi-center trial was conducted worldwide. The overall time to participate in this study is up to 3 years. Participants will make multiple visits to the clinic, and 3 months after the End-of-Treatment visit. Follow-up is intended to continue for 2 years after the last participants was enrolled into the study.

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