Erlotinib hydrochloride Basic information
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Product Name: |
Erlotinib hydrochloride |
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Synonyms: |
ERLOTINIB HCL;ERLOTINIB HCL SALT;ERLOTINIB HCL SALT :TARCEVA;Erlotinib, Hydrochloride Salt;N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, Hydrochloride Salt, OSI 774, Tarceva;N-(3-Ethynylphenyl)-6,7-bis-(2-methoxyethoxy)-quinazolin-4-amine;[6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4yl]-(3-ethynyl-phenyl)-amine;Tarceva HydrochlorideSee E625000 |
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CAS No: |
183319-69-9 |
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MF: |
C22H24ClN3O4 |
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MW: |
429.9 |
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EINECS: |
620-491-0 |
Erlotinib hydrochloride Chemical Properties
| Melting point | 223-225°C |
| Boiling point | 553.6ºC at 760mmHg |
| storage temp. | Inert atmosphere,Store in freezer, under -20°C |
| solubility | Soluble in DMSO (up to 18 mg/ml with warming). |
| pka | pKa (25°): 5.42 |
| form | Yellow powder. |
| color | White or off-white |
| Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Erlotinib hydrochloride Usage And Synthesis
| Chemical Properties | Off-White Solid |
| Originator | Pfizer(US) |
| Uses | Erlotinib hydrochloride (V), a quinazoline derived small molecule inhibitor of epidermal growth factor receptor (EDGFR) tyrosine kinase, was approved in November, 2004, for the treatment of advanced or metastatic non-smallcell lung cancer. It belongs to the same class as gefitinib,another quinazoline approved for treatment of advanced lung cancer, but with improved pharmacokinetic properties. The molecule was originated by Pfizer and development initiated in collaboration with OSI, which assumed full rights to the drug when Pfizer merged with Warner Lambert. Subsequently, Genentech/Roche went into licensing agreement with OSI to develop and market the drug in the US and Worldwide. |
It is the hydrochloride of the molecularly targeted drug erlotinib. The U.S. Food and Drug Administration (FDA) has approved erlotinib (Tarceva) combined with gemcitabine as the first-line treatment for locally advanced and metastatic pancreatic cancer. The small molecule compound erlotinib is a receptor tyrosine kinase inhibitor. It inhibits the phosphorylation reaction by competitively binding with adenosine triphosphate to the catalytic site of the receptor tyrosine kinase in the cell, thereby blocking the It has proliferation signal transduction, inhibits the activity of tumor cell ligand-dependent HER-1/EGFR, and achieves the effect of inhibiting tumor cell proliferation. It is also another tyrosine kinase inhibitor used in the treatment of NSCLC.
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