1508250-72-3

Basic information

• Product Name: EGF816 (mesylate)
• Synonyms: EGF816 (mesylate)
• CAS NO: 1508250-72-3
• Molecular Formula: C27H35ClN6O5S
• Molecular Weight: 591.122
• Mol File: 1508250-72-3.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• CAS DataBase Reference: EGF816 (mesylate)(CAS DataBase Reference)
• NIST Chemistry Reference: EGF816 (mesylate)(1508250-72-3)
• EPA Substance Registry System: EGF816 (mesylate)(1508250-72-3)

Safety Data

• Hazardous Substances Data: 1508250-72-3(Hazardous Substances Data)

Usage

General Description

EGF816 (mesylate) is a small molecule inhibitor that specifically targets the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. By binding to and inhibiting the activity of EGFR, EGF816 mesylate may disrupt EGFR signal transduction pathways, thereby inhibiting tumor cell growth and proliferation. This targeted therapy may be more effective and less toxic than traditional chemotherapy for patients with EGFR-mutant non-small cell lung cancer (NSCLC). EGF816 mesylate is still undergoing clinical trials to determine its efficacy and safety as a potential treatment option for NSCLC and other EGFR-mutated cancers.

Upstream product

• 75-75-2 methanesulfonic acid 
• 1508256-20-9 (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide 
• 4021-11-8 2-methylisonicotinic acid 

Relevant articles and documents

METHODS FOR TREATING EGFR MUTANT CANCERS

The present invention is directed to methods for the treatment of EGFR mutant cancer. In one embodiment, the cancer is non-small cell lung cancer (NSCLC) wherein the tumor harbors the activating EGFR mutations (e.g., L858R and ex19del) and/or the acquired/resistant "gatekeeper" T790M mutation.

EGFR INHIBITOR FORMS

The present disclosure generally discloses polymorphic forms of (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3- yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (Compound EGFRi). A pharmaceutical composition comprising the form(s), as well of methods of using the form(s) in the treatment of cancer indication, and methods for obtaining such forms are also disclosed.

EGFR INHIBITOR FORMS

The present disclosure generally relates to polymorphic form(s) of 184 (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2 -yl)-2-methylisonicotinamide (Compound EGFRi). The present disclosure also generally relates to a pharmaceutical composition comprising the form(s), as well of methods of using the form(s) in the treatment of cancer indications, and methods for obtaining such forms.