1020172-07-9

Usage

Uses

Used in Pharmaceutical Industry:
Rebastinib is used as a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, respectively. It also inhibits the Src family kinases Src, Lyn, Fgr, and Hck, as well as the tyrosine kinases KDR, FLT3, and Tie2 at nanomolar concentrations. Rebastinib is used for its marked inhibition of CML cell lines compared to non-CML leukemia lines, making it a potential therapeutic agent for certain types of cancer.
Used in COVID-19 Research:
Rebastinib is used as a COVID-19-related research product, contributing to the development of treatments and therapies for the disease.
Used in Cancer Treatment:
Rebastinib inhibits mutant Abl1T315I signaling and prolongs survival in a mouse Ba/F3 cell allograft model. It also exhibits in vivo antineoplastic activity against cells with the T674I point mutation of FIP1-like-1-platelet-derived growth factor receptor α, making it a potential treatment option for certain types of cancer.

references

[1] chan w w, wise s c, kaufman m d, et al. conformational control inhibition of the bcr-abl1 tyrosine kinase, including the gatekeeper t315i mutant, by the switch-control inhibitor dcc-2036. cancer cell, 2011, 19(4): 556-568.

Upstream product

• 757251-39-1 4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide 
• 1011464-72-4 2,2,2-trichloroethyl (3-(tert-butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)carbamate 
• 580-16-5 6-hydroxyquinoline 
• 173089-80-0 quinolin-6-yl triflate 
• 98-98-6 2-Picolinic acid 
• 53750-66-6 4-chloro-pyridine-2-carbonyl chloride 
• 220000-87-3 4-chloro-N-methylpicolinamide 
• 399-95-1 4-amino-3-fluorophenol 
• 897373-62-5 5-tert-butyl-2-quinolin-6-yl-2H-pyrazol-3-ylamine 
• 59997-51-2 trimethylacetylacetonitrile 
• 1012879-55-8 1-(diphenylmethylene)-2-(quinolin-6-yl)hydrazine 

Relevant academic research and scientific papers

METHODS OF USING REBASTINIB IN THE TREATMENT OF DISORDERS

Described herein are methods of treating various disorders in patients in need thereof, comprising administering to the patient the compound of Formula (I) or a pharmaceutically acceptable salt thereof. Exemplary disorders that can be treated by the methods described herein include gynecologic carcinosarcomas, endometrial adenocarcinomas, mesotheliomas, ovarian cancers, pancreatic ductal adenocarcinomas, and lung cancers.

METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES

Compounds of the present invention find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites secondary sites, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, thyroid cancer, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, i.e. diabetic retinopathy and age-related macular degeneration, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, human inflammation, rheumatoid spondylitis, ostero-arthritis, asthma, gouty arthritis, sepsis, septic shock, endotoxic shock, Gram-negative sepsis, toxic shock syndrome, adult respiratory distress syndrome, stroke, reperfusion injury, neural trauma, neural ischemia, psoriasis, restenosis, chronic obstructive pulmonary disease, bone resorptive diseases, graft-versus-host reaction, Crohn's disease, ulcerative colitis, inflammatory bowel disease, pyresis, and combinations thereof, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-KIT kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, VEGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, PDGFR kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, FLT-3 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TIE-2 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, TRK kinases, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, c-MET kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a HER kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES

The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.