1020172-07-9 Usage
Description
N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea, also known as Rebastinib (DCC-2036), is an orally bioavailable tyrosine kinase inhibitor. It is a conformational control inhibitor of Abl1 and Abl1-T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and shows low activity towards c-Kit. It is currently in Phase 1 and is a COVID-19-related research product.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1020172-07-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,2,0,1,7 and 2 respectively; the second part has 2 digits, 0 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1020172-07:
(9*1)+(8*0)+(7*2)+(6*0)+(5*1)+(4*7)+(3*2)+(2*0)+(1*7)=69
69 % 10 = 9
So 1020172-07-9 is a valid CAS Registry Number.
1020172-07-9Relevant articles and documents
METHODS OF USING REBASTINIB IN THE TREATMENT OF DISORDERS
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, (2021/09/10)
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.
KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
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Page/Page column 49, (2008/06/13)
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.
