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OSI 420
- 6-O-Desmethyl-erlotinib
- Soluble in DMSO
- MF: C21H21N3O4
- MW: 379.41
Description
An active O-desmethyl metabolite of Erlotinib (Axon 1128), which inhibits EGFR tyrosine kinase; precursor of [11C]-labelled Erlotinib for PET study
More Information
| Parent CAS No. | 183321-86-0 |
|---|---|
| Chemical Name | 2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol |
| SMILES | N(C1C=CC=C(C#C)C=1)C1=NC=NC2=CC(OCCOC)=C(OCCO)C=C12 |
| MFCD | N.A. |
| InChi | InChI=1S/C21H21N3O4/c1-3-15-5-4-6-16(11-15)24-21-17-12-19(27-8-7-25)20(28-10-9-26-2)13-18(17)22-14-23-21/h1,4-6,11-14,25H,7-10H2,2H3,(H,22,23,24) |
| InChiKey | KOQIAZNBAWFSQM-UHFFFAOYSA-N |
| CID | 10317566 |
| Short Description | EGFR inhibitor |
References
- A Broniscer et al. Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420. Clin. Cancer Res. 2007, 13(5), 1511-1515.
- Y Togashi et al. Cerebrospinal Fluid Concentration of Erlotinib and its Active Metabolite OSI-420 in Patients with Central Nervous System Metastases of Non-small Cell Lung Cancer. J. Thoracic Oncol. 2010, 5(7), 950-955.
- I. Bahce et al. Development of [(11)C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status. Clin. Cancer Res. 2013, 19, 183-193.
- NF Smith et al. Modulation of erlotinib pharmacokinetics in mice by a novel cytochromeP450 3A4 inhibitor, BAS 100. Br. J. Cancer 2008, 98, 1630–1632.
- AA Memon et al. Positron Emission Tomography (PET) Imaging with [11C]-Labeled Erlotinib: A Micro-PET Study on Mice with Lung Tumor Xenografts. Cancer Res. 2009, 69(3), 873-878.
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