|N-(4-((3-氯-4-氟苯基)氨基)-7-(3-甲基-3-(4-甲基哌嗪-1-基)丁-1-炔-1-基)喹唑啉-6-基)丙烯酰胺|CsnPharm

CAS No.: 451492-95-8

N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide Catalog No. CSN16123

Synonyms: MP-412 free base;AV-412 Free Base

AV-412 is an inhibitor of EGFR (IC50 = 0.5-2 nM), ErbB2 (IC50=19 nM), Abl receptor (IC50 = 41nM), mutant EGFR-L858R (IC50=0.51 nM) and EGFR-T790M (IC50=0.79 nM). It also inhibits autophosphorylation of EGFR and ErbB2 with IC50s of 43 nM and 282 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR (L858R)

IC50:0.51nM EGFR (T790M)

IC50:0.79nM HER2

IC50:19nM
描述AV-412 is a potent dual inhibitor of EGFR and ErbB2 (IC50=19 nM) tyrosine kinases, including the mutant EGFR (L858R IC50=0.51 nM, T790M IC50=0.79 nM). It inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00381654	Tumor	Phase 1	Terminated(Study did not meet ... more >>pre-specified objectives.) Collapse <<	-	United States, Maryland ... more >> Johns Hopkins University School of Medicine Baltimore, Maryland, United States, 21205 Argentina Hospital Universitatrio Austral Buenos Aires, Argentina Instituto Médico Especializado Alexander Fleming Buenos Aires, Argentina Collapse <<
NCT00551850	Advanced Cancer ... more >> Refractory Cancer Collapse <<	Phase 1	Completed	-	United States, District of Col... more >>umbia Georgetown University Hospital Washington, District of Columbia, United States, 20007 United States, Kansas Kansas Masonic Cancer Research Center Kansas City, Kansas, United States, 66160 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, New York Montefiore Medical Center New York City, New York, United States, 10461 Collapse <<

参考文献

[1] Suzuki T, Fujii A, et al. Ubiquitination and downregulation of ErbB2 and estrogen receptor-alpha by kinase inhibitor MP-412 in human breast cancer cells. J Cell Biochem. 2011 Sep;112(9):2279-86.
[2] Suzuki T, Fujii A, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9724 mL
- 9.8619 mL
- 19.7238 mL
- 5 mM
- 0.3945 mL
- 1.9724 mL
- 3.9448 mL
- 10 mM
- 0.1972 mL
- 0.9862 mL
- 1.9724 mL

技术信息

CAS号

451492-95-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H28ClFN6O

运输

蓝冰

分子量

507.00

别名

MP-412 free base;AV-412 Free Base

溶解度

DMSO	49.0 mg/mL (96.6 mM)

动物实验配方

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靶点	Description	IC50
EGFR (L858R)		IC50:0.51nM
EGFR (T790M)		IC50:0.79nM
HER2		IC50:19nM

N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide Catalog No. CSN16123

靶点选择性

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