Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM.

Product information

CAS Number: 183319-69-9

Molecular Weight: 429.90

Formula: C22H24ClN3O4

Synonym:

CP-358774

CP358774

OSI-774

OSI 774

OSI774

Tarceva

CP-358, 774

Related CAS Number:

183321-74-6 (Erlotinib free base)

248594-19-6 (Erlotinib mesylate)

Chemical Name: N-(3-ethynylphenyl)-6, 7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride

Smiles: Cl.COCCOC1=CC2=NC=NC(NC3=CC(=CC=C3)C#C)=C2C=C1OCCOC

InChiKey: GTTBEUCJPZQMDZ-UHFFFAOYSA-N

InChi: InChI=1S/C22H23N3O4.ClH/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 4 mg/mLwarmed(9.3 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon cancer cells. Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition.

In Vivo:

At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate.

References:

1. Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.
2. Li T, et al. Clin Cancer Res, 2007, 13(11), 3413-3422.
3. Ali S, et al. Mol Cancer Ther, 2008, 7(6), 1708-1719.
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6. Furugaki K,et al. Oncol Lett. 2010, 1(2), 231-235.
7. Bago-Horvath Z, et al. 2012, DOI: 10.1159/000337257

Products are for research use only. Not for human use.