OSI-420 Property

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 and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

OSI-420 Chemical Properties,Usage,Production

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 JAK2^V617F 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.

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.

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.