183319-69-9 Erlotinib HCl (OSI-744) AKSci M375
 
 
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  M375    
Erlotinib HCl (OSI-744)
, 98% (HPLC)
 
Tarceva




IDENTITY
CAS Number:183319-69-9
MDL Number:MFCD07781272
MF:C22H24ClN3O4
MW:429.9
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:228-235°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO: 3mg/mL; H2O: <1mg/mL; EtOH: <1mg/mL
Application(s):HER1/EGFR inhibitor
Form:HCl salt

REVIEW

 Erlotinib is an EGFR inhibitor. The drug follows Iressa (gefitinib), which was the first drug of this type. Erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.[1] For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. By inhibiting the ATP, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.

REFERENCES
[1]Raymond E, Faivre S, Armand J (2000). Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs 60 Suppl 1: 15-23; discussion 41-2. PMID 11129168.
[2] 2009 - SATURN: A double-blind, randomized, phase III study of maintenance erlotinib versus placebo following nonprogression with first-line platinum-based chemotherapy in patients with advanced NSCLC.
[3] Erlotinib for Advanced NSCLC is Marginally Cost Effective, Fran Lowry, Medscape, 25 February 2010.
[4] Takimoto CH, Calvo E. Principles of Oncologic Pharmacotherapy in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


RELATED PRODUCTS
M375Erlotinib HCl (OSI-744)
P443Erlotinib

Current as of June 22, 2024


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CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


PubChem