Erlotinib hydrochloride
- CAS NO.:183319-69-9
- Empirical Formula: C22H24ClN3O4
- Molecular Weight: 429.9
- MDL number: MFCD07781272
- EINECS: 620-491-0
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-05-21 14:26:55
What is Erlotinib hydrochloride ?
Description
Erlotinib, launched as once daily oral treatment for patients with non-small-cell lung cancer (NSCLC), is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, and it is the second small-molecule drug to be marketed with this mechanism of action. Both erlotinib and its predecessor, gefitinib, are members of the anilinoquinazoline class of tyrosine kinase inhibitors. They compete with the binding of ATP to the intracellular tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and blocking downstream signal transduction.
The Uses of Erlotinib hydrochloride
Erlotinib Hydrochloride is a HER-1/EGFR tyrosine kinase inhibitor with anti-neoplastic properties, competitive with ATP. 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.
in vitro
In vitro, Erlotinib inhibits purified human EGFR tyrosine kinase with an IC50 of 2 nM and blocks EGFR autophosphorylation in cellular assays with an IC50 of 20nM. Treatment of human colon cancer cells with erlotinib was associated with growth inhibition, G1 cell cycle arrest, and apoptosis. Oral administration of erlotinib in athymic mice produced potent antitumor effects with an ED50 of 9.2 mg/kg/day for HN5 head and neck xenografts and 14 mg/ kg/day for A431 epidermoid xenografts.
Production
Erlotinib is prepared by the condensation of 3-ethynylaniline with 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline, which is a key intermediate obtained in five synthetic steps starting from ethyl 3,4- dihydroxybenzoate.
Properties of Erlotinib hydrochloride
Melting point: | 223-225°C |
storage temp. | Inert atmosphere,Store in freezer, under -20°C |
solubility | Soluble in DMSO (up to 18 mg/ml with warming). |
form | Yellow powder. |
color | White or off-white |
Safety information for Erlotinib hydrochloride
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H413:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. |
Computed Descriptors for Erlotinib hydrochloride
Abamectin manufacturer
Jigs Chemical ltd
Alembic Pharmaceuticals Limited
Shilpa Medicare Limited (SML)
Vannsh Life Sciences Pvt Ltd
Zyphars Biopharmaceuticals Pvt. Ltd
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