OSI-420
- CAS NO.:183321-86-0
- Empirical Formula: C21H21N3O4
- Molecular Weight: 379.41
- MDL number: MFCD09841129
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-09 19:38:33
What is OSI-420?
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.
Chemical properties
Off-White Solid
The Uses of OSI-420
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.
The Uses of OSI-420
A metabolite of Erlotinib (E625000), an anti cancer agent.
What are the applications of Application
OSI-420, Free Base (Desmethyl Erlotinib) is a metabolite of Erlotinib
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.
Properties of OSI-420
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 |
Safety information for OSI-420
Computed Descriptors for OSI-420
New Products
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