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Linagliptin Home您现在的位置:HOME >> PRODUCTS >> Medicine Active ingredient

Linagliptin

所属类别:Medicine Active ingredient 点击次数:539次 发布时间:2017-04-13

Linagliptin
详情
 Linagliptin Basic Info.
Synonyms: 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione; 8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione; 1h-purine-2,6-dione, 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-
CAS:668270-12-0
MW: 472.5422
MF:C25H28N8O2
Density: 1.398g/cm3
Melting Point(ºC): 202ºC
Boiling Point(ºC): 661.189°C at 760 mmHg
Flash Point(ºC): 353.675°C
refractive_index: 1.717
 
 
Product Name: Crizotinib
Synonyms: PF-2341066; 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-Pyridinamine;(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine;3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]pyridin-2-amine;Crizotinib;PF 2341066;PF-02341066;PF-2341066/Crizotinib;3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine 
CAS: 877399-52-5 
MF: C21H22Cl2FN5O 
MW: 450.343 
Purity: 99%
Appearance: White Crystalline Powder
 
Description :
 
Crizotinib is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor, approved for treatment of some non-small cell lung carcinoma (NSCLC) in the US and some other countries, and undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, and other advanced solid tumors in both adults and children.
 
 
 
2. What is Crizotinib:
 
Crizotinib (trade name Xalkori,) is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor, approved for treatment of some non-small cell lung carcinoma (NSCLC) in the US and some other countries, and undergoing clinical trials testing its safety and efficacy inanaplastic large cell lymphoma, neuroblastoma, and other advanced solid tumors in both adults and children.
 
3. How does Crizotinib works:
 
Crizotinib has an aminopyridine structure, and functions as a protein kinase inhibitor by competitive binding within the ATP-binding pocket of target kinases. About 4% of patients with non-small cell lung carcinoma have a chromosomal rearrangement that generates a fusion genebetween EML4 ('echinoderm microtubule-associated protein-like 4') andALK ('anaplastic lymphoma kinase'), which results in constitutivekinase activity that contributes to carcinogenesis and seems to drive the malignant phenotype. The kinase activity of the fusion protein is inhibited by crizotinib. Patients with this gene fusion are typically younger non-smokers who do not have mutations in either theepidermal growth factor receptor gene (EGFR) or in the K-Ras gene.The number of new cases of ALK-fusion NSLC is about 9,000 per year in the U.S. and about 45,000 worldwide.
 
4. Crizotinib is used for:
 
Treating certain types of lung cancer. It may also be used for other conditions as determined by your doctor.
 
Crizotinib is a tyrosine kinase inhibitor. It works by preventing the growth of cancer cells.
 
Crizotinib inhibits the c-Met/Hepatocyte growth factor receptor (HGFR) tyrosine kinase, which is involved in the oncogenesis of a number of other histological forms of malignant neoplasms.
 
Crizotinib is currently thought to exert its effects through modulation of the growth, migration, and invasion of malignant cells.Other studies suggest that crizotinib might also act via inhibition of angiogenesis in malignant tumors.

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