WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 401565
CAS#: 183321-86-0
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.
MedKoo Cat#: 401565
Name: OSI-420
CAS#: 183321-86-0
Chemical Formula: C21H21N3O4
Exact Mass: 379.15321
Molecular Weight: 379.40914
Elemental Analysis: C, 66.48; H, 5.58; N, 11.08; O, 16.87
Related CAS #: 183320-51-6 (HCl); 183321-86-0
Synonym: OSI420; OSI-420; OSI 420; CP473420; CP-473420; CP 473420; Desmethyl Erlotinib.
IUPAC/Chemical Name: 2-[[4-[(3-Ethynylphenyl)amino]-7-(2-methoxyethoxy)-6-quinazolinyl]oxy]ethanol
InChi Key: KOQIAZNBAWFSQM-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCO
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not soluble in water.
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 379.40914 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Masago K, Togashi Y, Fukudo M, Terada T, Irisa K, Sakamori Y, Kim YH, Mio T, Inui K, Mishima M. Plasma and pleural fluid pharmacokinetics of erlotinib and its active metabolite OSI-420 in patients with non-small-cell lung cancer with pleural effusion. Clin Lung Cancer. 2011 Sep;12(5):307-12. doi: 10.1016/j.cllc.2011.06.004. Epub 2011 Jul 19. PubMed PMID: 21775215.
2: Togashi Y, Masago K, Fukudo M, Terada T, Fujita S, Irisa K, Sakamori Y, Kim YH, Mio T, Inui K, Mishima M. 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 Thorac Oncol. 2010 Jul;5(7):950-5. PubMed PMID: 20479691.
3: Togashi Y, Masago K, Fukudo M, Terada T, Ikemi Y, Kim YH, Fujita S, Irisa K, Sakamori Y, Mio T, Inui K, Mishima M. Pharmacokinetics of erlotinib and its active metabolite OSI-420 in patients with non-small cell lung cancer and chronic renal failure who are undergoing hemodialysis. J Thorac Oncol. 2010 May;5(5):601-5. PubMed PMID: 20234322.
4: Meany HJ, Fox E, McCully C, Tucker C, Balis FM. The plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite (OSI-420) after intravenous administration of erlotinib in non-human primates. Cancer Chemother Pharmacol. 2008 Aug;62(3):387-92. Epub 2007 Oct 12. PubMed PMID: 17932674.
5: Broniscer A, Panetta JC, O'Shaughnessy M, Fraga C, Bai F, Krasin MJ, Gajjar A, Stewart CF. Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420. Clin Cancer Res. 2007 Mar 1;13(5):1511-5. PubMed PMID: 17332296.
6: Masters AR, Sweeney CJ, Jones DR. The quantification of erlotinib (OSI-774) and OSI-420 in human plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Apr 1;848(2):379-83. Epub 2006 Nov 13. PubMed PMID: 17101305.
7: Zhang W, 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. PubMed PMID: 15607718.
8: Zhao M, He P, Rudek MA, Hidalgo M, Baker SD. Specific method for determination of OSI-774 and its metabolite OSI-420 in human plasma by using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Aug 15;793(2):413-20. PubMed PMID: 12906916.
