915942-22-2

Basic information

• Product Name: Neratinib Maleate
• Synonyms: Neratinib Maleate;(E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide maleate
• CAS NO: 915942-22-2
• Molecular Formula: C34H33ClN6O7
• Molecular Weight: 673.11482
• EINECS: -0
• Mol File: 915942-22-2.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Storage Temp.: Inert atmosphere,Room Temperature
• CAS DataBase Reference: Neratinib Maleate(CAS DataBase Reference)
• NIST Chemistry Reference: Neratinib Maleate(915942-22-2)
• EPA Substance Registry System: Neratinib Maleate(915942-22-2)

Safety Data

• Hazardous Substances Data: 915942-22-2(Hazardous Substances Data)

Usage

Description

Neratinib Maleate, also known as HKI-272, is a potent pan-HER inhibitor and an irreversible tyrosine kinase inhibitor. It effectively binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, including EGFR (HER1), HER2, and HER4. This action leads to a reduction in the phosphorylation and activation of downstream signaling pathways, making it a promising candidate for cancer treatment.

Uses

Used in Oncology:
Neratinib Maleate is used as an anticancer drug for the treatment of adults with certain types of HER2-positive breast cancer that have already been treated. It is also being studied for its potential in treating other types of cancer. By blocking specific proteins, Neratinib Maleate helps prevent the growth of cancer cells and may even induce their death. It is classified as a tyrosine kinase inhibitor.
Used in Drug Development:
Neratinib Maleate is utilized as a codrug in the preparation of heterobifunctional proteolysis-targeting chimera (PROTAC) compounds. These compounds serve as degraders of estrogen receptors, offering a novel approach to target and degrade specific proteins within cells, which can be beneficial in the treatment of various diseases, including cancer.

Biological Activity

Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours.

Mechanism of action

Neratinib Maleate is the maleate salt form of neratinib, an orally available, quinazoline-based, irreversible inhibitor of both the receptor tyrosine kinases (RTKs) human epidermal growth factor receptor 2 (HER2; ERBB2) and human epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, neratinib targets and covalently binds to the cysteine residue in the ATP-binding pockets of both HER2 and EGFR. This inhibits their activity and results in the inhibition of downstream signal transduction events, induces cell cycle arrest, apoptosis and ultimately decreases cellular proliferation in HER2- and EGFR-expressing tumor cells. EGFR and HER2, RTKs that are mutated or overactivated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.