| Identification | Back Directory | [Name]
OSI-420 | [CAS]
183321-86-0 | [Synonyms]
OSI-420
CP 373420
OSI-420 (free base)
ROSCOVITINE(CVC202)
Erlotinib iMpurity H
Erlotinib impurity J
Erlotinib impurity N
6-O-Desmethyl Erlotinib 1
Erlotinib O-DesMethyl Metabolite
Desmethyl Erlotinib (CP-473420, OSI-420)
2-((4-((3-Ethynylphenyl)amino)-7-(2-methoxyethoxy)quinazolin-6-yl)oxy)ethanol
2-((4-((3-ethynylphenyl)amino)-7-(2-methoxyethoxy)quinazolin-6-yl)oxy)ethan-1-ol | [Molecular Formula]
C21H21N3O4 | [MDL Number]
MFCD09841129 | [MOL File]
183321-86-0.mol | [Molecular Weight]
379.409 |
| Chemical Properties | Back Directory | [Melting point ]
140-142°C | [density ]
1.30 | [storage temp. ]
-20°C Freezer | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥51 mg/mL in DMSO | [form ]
A crystalline solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Solid | [Uses]
A metabolite of Erlotinib (E625000), an anti cancer agent. | [Uses]
OSI-420 (Desmethyl Erlotinib,CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells.
| [Description]
Desmethyl erlotinib is a metabolite of erlotinib . 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. | [References]
[1] zhang w1, siu ll, moore mj, chen ex.simultaneous determination of osi-774 and its major metabolite osi-420 in human plasma by using hplc with uv detection. j chromatogr b analyt technol biomed life sci. 2005 jan 5;814(1):143-7.
[2] bonomi p. erlotinib: a new therapeutic approach for non-small cell lung cancer.expert opin investig drugs. 2003 aug;12(8):1395-401. |
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