OSI-420 - CAS 183320-51-6
Catalog number: B0084-286627
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
EGFR
Description:
OSI-420 (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.
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Synonyms:
OSI-420; CP-473420; Desmethyl Erlotinib.
MSDS:
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Application:
For research used only
1.A validated liquid chromatography tandem mass spectrometry method for quantification of erlotinib, OSI-420 and didesmethyl erlotinib and semi-quantification of erlotinib metabolites in human plasma.
Svedberg A1, Gréen H2, Vikström A3, Lundeberg J4, Vikingsson S5. J Pharm Biomed Anal. 2015 Mar 25;107:186-95. doi: 10.1016/j.jpba.2014.12.022. Epub 2014 Dec 25.
A liquid chromatography tandem mass spectrometry method was developed and validated for quantification of erlotinib and its metabolites in human plasma. The method is suitable for therapeutic drug monitoring and pharmacokinetic studies. The substances were extracted using protein precipitation, separated on a BEH XBridge C18 column (100 ×2.1 mm, 1.7 μm) by gradient elution at 0.7 mL/min of acetonitrile and 5 mM ammonium acetate. The concentration was determined using a Waters Xevo triple quadrupole mass spectrometer in a multi reaction monitoring mode. The total run time was 7 min. Deuterated erlotinib and OSI-597 were used as internal standard for erlotinib and its metabolites, respectively. Erlotinib, OSI-420 and didesmethyl erlotinib were quantified in the concentration range 25-5000 ng/mL, 0.5-500 ng/mL and 0.15-10 ng/mL, respectively. Precision and accuracy was <14% except for OSI-420 at LLOQ (17%). Extraction recovery was above 89%, 99% and 89% for erlotinib, OSI-420 and didesmethyl erlotinib, respectively.
2.A phase 1 study of OSI-930 in combination with erlotinib in patients with advanced solid tumours.
Macpherson IR1, Poondru S, Simon GR, Gedrich R, Brock K, Hopkins CA, Stewart K, Stephens A, Evans TR. Eur J Cancer. 2013 Mar;49(4):782-9. doi: 10.1016/j.ejca.2012.09.036. Epub 2012 Oct 22.
AIM: To determine the maximum tolerated dose (MTD) of OSI-930 that can be combined with erlotinib, and establish recommended phase 2 doses when both agents are administered daily in patients with advanced solid tumours.
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CAS 183320-51-6 OSI-420

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