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

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

Uses

Used in Pharmaceutical Industry:
EGF816 (mesylate) is used as an antineoplastic agent for the treatment of EGFR-mutant non-small cell lung cancer (NSCLC) due to its ability to inhibit EGFR signal transduction pathways, thereby disrupting tumor cell growth and proliferation.
Used in Clinical Research:
EGF816 (mesylate) is used as a subject of clinical trials to determine its efficacy and safety as a potential treatment option for NSCLC and other EGFR-mutated cancers, offering a targeted therapy approach that may be more effective and less toxic than traditional chemotherapy.

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

THERAPEUTIC COMBINATION FOR THE TREATMENT OF CANCER

This invention relates to a pharmaceutical combination comprising (a) an EGFR inhibitor and (b) a FGFR inhibitor, particularly for use in the treatment of a cancer. This invention also relates to uses of such combination for preparation of a medicament for the treatment of a cancer; methods of treating or preventing a cancer in a subject in need thereof comprising administering to said subject a jointly therapeutically effective amount of said combination; pharmaceutical compositions comprising such combination and commercial packages thereto.

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.

FORMS OF THE EGFR INHIBITOR

The present disclosure generally relates to polymorphic form(s) 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). 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.

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.

COMPOUNDS AND COMPOSITIONS FOR MODULATING EGFR ACTIVITY

The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.