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ErlotinibEGFR tyrosine kinase inhibitor

Erlotinib

Catalog No. A3397
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
100mg $50.00 In stock
500mg $70.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Erlotinib

Related Biological Data

Erlotinib

Related Biological Data

Erlotinib

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Chemical Properties

Cas No. 183321-74-6 SDF Download SDF
Synonyms NSC 718781;OSI-744;R-1415;OSI744;OSI 744;R1415;R 1415
Chemical Name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
Canonical SMILES COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
Formula C22H23N3O4 M.Wt 393.44
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Erlotinib (also known as NSC 718781 or CP 358,774) is a potent and orally-bioavailable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase that selectively and reversibly inhibits EGFR-associated intracellular autophosphorylation of tyrosine kinase. Erlotinib inhibits purified EGFR tyrosine kinase and EGFR autophosphorylation intact cells with 50% inhibition concentration IC50 values of 2 nmol/L and 20 nmol/L respectively. Erlotinib competes for the ATP-binding sits on the intracellular domain of EGFR resulting in the inhibition of downstream signaling pathway involved in angiogenesis, cell propagation and cell survival. Erlotinib concentration-dependently inhibits EGFR-mediated propagation signals transduction, displays prominent anti-tumor activity against neoplasms harboring EGFR expression and exhibits a tolerable toxicologic profile.

Reference

Janine Smith. Erlotinib: small-molecule targeted therapy in the treatment of non-small-cell lung cancer. Clinical Therapeutics 2005; 27(10): 1513-1534