Erlotinib D6 HCl Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO: slightly, heated,Methanol: slightly soluble

form 

A solid

color 

White to off-white

Erlotinib D6 HCl Usage And Synthesis

Description

Erlotinib-d₆ (hydrochloride) contains six deuterium atoms located on the methoxy group. It is intended for use as an internal standard for the quantification of erlotinib by GC- or LC-MS. Erlotinib is a tyrosine kinase inhibitor that 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 JAK2^V617F (IC₅₀ = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib are used to treat certain forms of cancer, including non-small cell lung cancer.

Uses

Erlotinib D6 HCl is a Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor, Antineoplastic.;Labeled Erlotinib, intended for use as an internal standard for the quantification of Erlotinib by GC- or LC-mass spectrometry.

References

[1] LUCA GIANNI  Giacomo G. Targeting the epidermal growth factor receptor a new strategy in cancer treatment.[J]. I supplementi di Tumori?: official journal of Societa italiana di cancerologia ... [et al.], 2002, 1 4: S60-1.
[2] J D MOYER. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase.[J]. Cancer research, 1997, 57 21: 4838-4848.
[3] ROY S HERBST  Paul A B. Targeting the epidermal growth factor receptor in non-small cell lung cancer.[J]. Clinical Cancer Research, 2003, 9 16 Pt 1: 5813-5824.

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