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Erlotinib

Erlotinib Structure
CAS No.
183321-74-6
Chemical Name:
Erlotinib
Synonyms
ERLOTINIB HCL;Tarceva;Erlortinib;R 1415;Rotini;OSI 744;Erlonat;ERLOTININ;ERLOTINIB;NSC-71878
CBNumber:
CB9285914
Molecular Formula:
C22H23N3O4
Molecular Weight:
393.44
MOL File:
183321-74-6.mol
MSDS File:
SDS
Modify Date:
2025/1/27 9:38:02

Erlotinib Properties

Melting point 159-160 °C
Boiling point 553.6±50.0 °C(Predicted)
Density 1.24
storage temp. Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form Solid
pka 5.32±0.30(Predicted)
color White
CAS DataBase Reference 183321-74-6(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Danger
Hazard statements  H350-H304-H227
Precautionary statements  P501-P202-P210-P201-P280-P370+P378-P331-P308+P313-P301+P310-P403+P235-P405
Safety Statements  24/25
HS Code  29335990
Hazardous Substances Data 183321-74-6(Hazardous Substances Data)

Erlotinib Chemical Properties,Uses,Production

Description

Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 μM). This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED50 value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 μM) and JAK2 mutant JAK2V617F positive hematopoietic progenitor cells (IC50 = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer.

Uses

Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.

Definition

ChEBI: A quinazoline compound having a (3-ethynylphenyl)amino group at the 4-position and two 2-methoxyethoxy groups at the 6- and 7-positions.

General Description

Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 60%
Elimination half-life = 36 h
Protein binding = 93%

Side effects

  • Burning, tingling, numbness or pain in the hands, arms, feet, or legs.
  • cough or hoarseness.
  • diarrhea (severe)
  • difficult or labored breathing.
  • fever or chills.
  • rash (severe)
  • sensation of pins and needles.
  • stabbing chest pain.

Synthesis

The synthesis of Erlotinib is as follows:
N-dimethylformamidine, 0.72 g (6.15 mmol) of N '- [2-cyano-4,5-bis (2-methoxyethoxy) phenyl] ) Of 3-aminophenylacetylene and 8 mL of acetic acid were reacted in a 50 mL reaction flask at 125 ° C for 1 hour and cooled to room temperature.20 mL of ice water was added to the mixture, the pH was adjusted to 10 with aqueous ammonia, and the mixture was stirred for 1 hour, suction filtered and the filter cake washed with water until neutral.The filter cake was dried to obtain 2.15 g of erlotinib in a yield of 91.5%.
synthesis of Erlotinib.png

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Erlotinib Spectrum

ERLOTINIB ERLOTINIB HCL SALT 4-[(3-ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline n-(3-ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine Erlotinib Hydrochloirde 4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)- ERLOTININ N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine Erlotinib & its intermediates CP-358774, Ro 50-8231 Erlotinib Free Base OSI 744 R 1415 Erlotinib &aMp its interMediates O-desmethyl erlotinib carboxylic acid Erlotinib N-(3-Ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine Erlotinib ERLOTINIB Erlotinib (OSI-744) Erlonat Erlotinib (Tarceva) NSC-71878 OSI744;CP-358774;NSC-71878;ERLOTINIB HCL (OSI 744;CP358774;NSC718781) Erlotinib USP/EP/BP Erlotinib (OSI744, Tarceva) ErlotinibQ: What is Erlotinib Q: What is the CAS Number of Erlotinib Q: What is the storage condition of Erlotinib Q: What are the applications of Erlotinib ERLOTINIB HCL Tarceva Erlortinib Erlotinib 183321-74-6 Rotini R-1415CP-358,774 Erlotinib (OSI-774) Noradrenaline Impurity 26 Erlotinib, 10 mM in DMSO 183321-74-6 83321-74-6 68304-21-3 2139253-68-1 Isotope Tarceva Anti-cancer&immunity Antineoplastic Inhibitors API APIs Pharmaceutical intermediate Erlotinib