1189953-78-3

Basic information

• Product Name: Erlotinib D6 HCl
• Synonyms: Erlotinib D6;Erlotinib Hydrochloride Impurity G
• CAS NO: 1189953-78-3
• Molecular Formula: C22H18ClD6N3O4
• Molecular Weight: 435.933630668
• Mol File: 1189953-78-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Erlotinib D6 HCl(CAS DataBase Reference)
• NIST Chemistry Reference: Erlotinib D6 HCl(1189953-78-3)
• EPA Substance Registry System: Erlotinib D6 HCl(1189953-78-3)

Safety Data

• Hazardous Substances Data: 1189953-78-3(Hazardous Substances Data)

Usage

Description

Erlotinib D6 HCl, also known as Erlotinib-d6 (hydrochloride), is a deuterated form of the tyrosine kinase inhibitor Erlotinib. It contains six deuterium atoms located on the methoxy group and is primarily used as an internal standard for the quantification of Erlotinib by gas chromatography (GC) or liquid chromatography-mass spectrometry (LC-MS). Erlotinib targets the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity and playing a significant role in the treatment of certain cancer types.

Uses

Used in Pharmaceutical Industry:
Erlotinib D6 HCl is used as an internal standard for the quantification of Erlotinib by GCor LC-MS, ensuring accurate measurement and analysis of the drug's concentration in various pharmaceutical formulations.
Used in Oncology Research:
Erlotinib D6 HCl is used as a Selective EGFR-tyrosine kinase inhibitor, playing a crucial role in antineoplastic therapy. It inhibits EGFR-associated kinase activity (IC50 = 2.5 μM), which helps in suppressing tumor growth in human head and neck carcinoma (HN5) tumor xenografts in mice with an ED50 value of 9 mg/kg.
Used in Cancer Treatment:
Erlotinib D6 HCl is used in the development of formulations containing Erlotinib, which are employed to treat certain forms of cancer, including non-small cell lung cancer. It also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 μM) and JAK2 mutant JAK2V617F (IC50 = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia.