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OSI-420

Names

[ CAS No. ]:
183320-51-6

[ Name ]:
OSI-420

[Synonym ]:
OSI-420
2-({4-[(3-Ethynylphenyl)amino]-7-(2-methoxyethoxy)-6-quinazolinyl}oxy)ethanol hydrochloride (1:1)
Desmethyl erlotinib hydrochloride
Ethanol, 2-[[4-[(3-ethynylphenyl)amino]-7-(2-methoxyethoxy)-6-quinazolinyl]oxy]-, hydrochloride (1:1)
S2205_Selleck
Desmethyl Erlotinib
Erlotinib Impurity 4

Biological Activity

[Description]:

Desmethyl Erlotinib (OSI-420) is an active metabolite of erlotinib, which is a potent EGFR tyrosin kinase inhibitor.

[Related Catalog]:

Research Areas >> Cancer

[In Vivo]

Desmethyl Erlotinib exposure (AUC) in plasma is 30% (range 12-59%) of erlotinib, and Desmethyl Erlotinib clearance is more than 5-fold higher than erlotinib. The CSF penetration of erlotinib and Desmethyl Erlotinib is <5% relative to total plasma concentration[1].

[References]

[1]. Meany HJ, et al. 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, 62(3), 387-392.


[Related Small Molecules]

Osimertinib (AZD9291) | Tyrphostin B42 (AG-490) | Neratinib (HKI-272) | Genistein | (-)-Epigallocatechin gallate | AG-1478 | Dacomitinib (PF-00299804) | Irbinitinib | Poziotinib | Olmutinib | Sapitinib | AZD-3759 | Pyrotinib | Canertinib dihydrochloride | BMS-690514

Chemical & Physical Properties

[ Molecular Formula ]:
C21H22ClN3O4

[ Molecular Weight ]:
415.870

[ Exact Mass ]:
415.129883

[ PSA ]:
85.73000

[ LogP ]:
3.62600

[ Storage condition ]:
-20℃

Related Compounds