Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H20BrN5O2.ClH |
Molecular Weight | 502.791 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC=C(Br)C=C1NC(=O)NC2=CC=CC3=C2C=CN3CC4=CC=NC(N)=C4
InChI
InChIKey=WWUKDILHPZKGIL-UHFFFAOYSA-N
InChI=1S/C22H20BrN5O2.ClH/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);1H
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
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26365907
200 mg twice daily dose level was declared as the maximum tolerated dose
Route of Administration:
Oral
Name | Type | Language | ||
---|---|---|---|---|
|
Code | English | ||
|
Code | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
44472553
Created by
admin on Fri Dec 15 17:34:52 GMT 2023 , Edited by admin on Fri Dec 15 17:34:52 GMT 2023
|
PRIMARY | |||
|
1441001-34-8
Created by
admin on Fri Dec 15 17:34:52 GMT 2023 , Edited by admin on Fri Dec 15 17:34:52 GMT 2023
|
NON-SPECIFIC STOICHIOMETRY | |||
|
7FM1I0S6F4
Created by
admin on Fri Dec 15 17:34:52 GMT 2023 , Edited by admin on Fri Dec 15 17:34:52 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD