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Description

CGI-1842 (also known as JI-101) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 that has been used in trials studying the treatment of Cancer, Colon Cancer, Neuroendocrine, Ovarian Cancer, and Advanced Solid Tumors. By targeting multiple angiogenesis signaling pathways in tumor vessel beds, CGI-1842 has the potential to inhibit multiple stages of tumor angiogenesis and thus enhance anti-tumor efficacy. In preclinical models, CGI-1842 induced concentration-dependent blocking of both EphB4- and VEGF-stimulated signaling pathways and has shown excellent antitumor activity. CGI-1842 is well tolerated in cancer patients and has shown impressive activity in Phase I clinical trials.

Approval Year

PubMed

PubMed

TitleDatePubMed
A pilot study of JI-101, an inhibitor of VEGFR-2, PDGFR-β, and EphB4 receptors, in combination with everolimus and as a single agent in an ovarian cancer expansion cohort.
2015 Dec
Patents

Patents

Sample Use Guides

In Vivo Use Guide
200 mg twice daily dose level was declared as the maximum tolerated dose
Route of Administration: Oral
Name Type Language
JI-101 HYDROCHLORIDE
Code English
CGI-1842 HYDROCHLORIDE
Code English
Code System Code Type Description
CAS
1441001-34-8
Created by admin on Tue Oct 22 00:56:29 UTC 2019 , Edited by admin on Tue Oct 22 00:56:29 UTC 2019
NON-SPECIFIC STOICHIOMETRY