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Details

Stereochemistry ACHIRAL
Molecular Formula C22H20BrN5O2
Molecular Weight 466.3309
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of JI-101

SMILES

COc1ccc(cc1NC(=Nc2cccc3c2ccn3Cc4cc[nH]c(=N)c4)O)Br

InChI

InChIKey=ZXBFYBLSJMEBEP-UHFFFAOYSA-N
InChI=1S/C22H20BrN5O2/c1-30-20-6-5-15(23)12-18(20)27-22(29)26-17-3-2-4-19-16(17)8-10-28(19)13-14-7-9-25-21(24)11-14/h2-12H,13H2,1H3,(H2,24,25)(H2,26,27,29)

HIDE SMILES / InChI

Molecular Formula C22H20BrN5O2
Molecular Weight 466.3309
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

200 mg twice daily dose level was declared as the maximum tolerated dose
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:24:59 UTC 2021
Edited
by admin
on Fri Jun 25 22:24:59 UTC 2021
Record UNII
980M4N37DH
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
JI-101
Code English
CGI-1842
Common Name English
ANGIOGENESIS INHIBITOR JI-101
Common Name English
UREA, N-(1-((2-AMINO-4-PYRIDINYL)METHYL)-1H-INDOL-4-YL)-N'-(5-BROMO-2-METHOXYPHENYL)-
Systematic Name English
Code System Code Type Description
ChEMBL
CHEMBL3545155
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY
DRUG BANK
DB12744
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY
PUBCHEM
11691242
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY
CAS
900573-88-8
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY
NCI_THESAURUS
C82413
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY NCIT
FDA UNII
980M4N37DH
Created by admin on Fri Jun 25 22:24:59 UTC 2021 , Edited by admin on Fri Jun 25 22:24:59 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY