950769-60-5

Usage

Uses

Used in Oncology:
GNE-493 is utilized as an anti-cancer agent for its ability to inhibit the Chk1 protein, which is pivotal in the regulation of the cell cycle and DNA repair. This inhibition can lead to the disruption of cancer cell proliferation and survival, making GNE-493 a promising treatment for various types of cancer.
Used in Combination Therapies:
Due to its selective targeting of Chk1, GNE-493 is considered for use in combination with other anti-cancer drugs. This approach aims to enhance the overall effectiveness of cancer treatment by leveraging the synergistic effects of multiple therapeutic agents, potentially overcoming drug resistance and improving patient outcomes.
Used in Personalized Cancer Therapies:
The specificity of GNE-493 for Chk1 suggests its potential application in personalized medicine, where treatments are tailored to the unique genetic and molecular characteristics of a patient's cancer. This precision approach may lead to more effective and less toxic treatments for cancer patients.
Used in Preclinical Cancer Research:
GNE-493 is extensively used in preclinical studies to explore its anti-cancer properties and to evaluate its safety and efficacy before moving into clinical trials. These studies are essential for understanding the compound's mechanism of action and its potential as a therapeutic agent in various cancer types, including lung, breast, and colon cancer.

InChI:InChI=1/C21H20N4O4S/c26-25(27)16-3-1-15(2-4-16)18-14-24-19-6-5-17(13-20(19)30-21(24)22-18)29-12-9-23-7-10-28-11-8-23/h1-6,13-14H,7-12H2

Upstream product

• 99-81-0 4-Nitrophenacyl bromide 
• 52481-41-1 4-(2-morpholinoethoxy)aniline 
• 65300-53-0 4-[2-(4-nitrophenoxy)ethyl]morpholine 
• 100-02-7 4-nitro-phenol 
• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 26278-79-5 2-amino-6-hydroxybenzothiazole 
• 914224-34-3 2-(4-nitrophenyl)imidazo[2,1-b][1,3]benzothiazol-7-ol 
• 3647-69-6 4-(2-chloroethyl)morpholine hydrochride 
• 3240-94-6 N-(2-chlorethyl)morpholine 

Downstream Products

• 950769-58-1 quizartinib 
• 1132827-21-4 Quizartinib dihydrochloride 
• 950769-61-6 2-(4-aminophenyl)-7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazole 

Relevant academic research and scientific papers

Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors

As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.

Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)

The invention discloses a benzoimidazo [2, 1-b] thiazole compound and application thereof, and belongs to the technical field of medicines. The inhibitory activity of the synthesized benzimidazo [2, 1-b] thiazole analogues on FLTT3 is more than 90%, wherein the compounds (compounds 2 , 4, 6, 8 and 10) are IC of FLTT3-ITD kinase. 50 Lower value, in particular compound 2, IC IC50 The value is only 5.60 nm, and therefore the compound of the present invention may be used as an inhibitor FLTT3, or for preparing a drug capable of modulating or suppressing diseases associated with abnormal cell proliferation by affecting the enzymatic activity of one or more tyrosine kinases and interfering with aberrant cell proliferation, having a wide application prospect. (by machine translation)

PROCESS FOR THE PREPARATION OF IMIDAZO[2,1-B][1,3]BENZOTHIAZOLE DERIVATIVES

Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)- N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-fe][l,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert- Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-and][l,3]benzo- thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers. N-(5-ferf-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl- ethoxy)imidazo[2,l-and][l,3]benzothiazol-2-yl]phenyl}urea is represented by the structure:

NEW AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY

The present invention concerns novel aminoacids derivatives, in particular some aminoacid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.

IMIDAZOLOTHIAZOLE COMPOUNDS AS MODULATORS OF PROTEIN KINASE

Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

SOLID FORMS COMPRISING N-(5-TERT-BUTYL-ISOXAZOL-3-YL)-N'-{4-[7-(2-MORPHOLIN-4-YL-ETHOXY)IMIDAZO[2,1-B][1,3]BENZOTHIAZOL-2-YL]PHENYL}UREA, COMPOSITIONS THEREOF, AND USES THEREWITH

Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin- 4-yl-ethoxy)imidazo[2,l-b][l,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatmen

Identification of N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2- morpholin-4-yl-ethoxy)imidazo-[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor

Treatment of AML patients with small molecule inhibitors of FLT3 kinase has been explored as a viable therapy. However, these agents are found to be less than optimal for the treatment of AML because of lack of sufficient potency or suboptimal oral pharma

Imidazolothiazole compounds for the treatment of disease

Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.