Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C33H30ClN5O3 |
| Molecular Weight | 580.076 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(=CC2=NN=C(NC3=CC=C(OCCN4CCCC4)C=C3)N=C12)C5=CC(OC(=O)C6=CC=CC=C6)=CC=C5Cl
InChI
InChIKey=JMGXJHWTVBGOKG-UHFFFAOYSA-N
InChI=1S/C33H30ClN5O3/c1-22-19-24(28-21-27(13-14-29(28)34)42-32(40)23-7-3-2-4-8-23)20-30-31(22)36-33(38-37-30)35-25-9-11-26(12-10-25)41-18-17-39-15-5-6-16-39/h2-4,7-14,19-21H,5-6,15-18H2,1H3,(H,35,36,38)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18311895Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18330892
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18311895
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/18330892
AGE-RELATED MACULAR DEGENERATION (AMD), PROLIFERATIVE DIABETIC RETINOPATHY (PDR) AND DIABETIC MACULAR EDEMA (DME) are collectively characterized by VEGF mediated retinal leakage, angiogenesis, and an underlying inflammatory process. TargeGen's TG100801 is designed to inhibit a select group of kinases involved in those three processes. Currently approved drug based therapy for macular degeneration requires repeated injection into the eye. TG100801 is the first topically applied, VEGFR)/Src kinase inhibitor to advance into the clinic for the treatment of Age-related macular degeneration, diabetic retinopathy. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. In cell based assays, following topical instillation, TG100572, the active drug produced by conversion of TG100801 as it penetrates the eye, was shown to induce apoptosis in proliferating endothelial cells responsible for neovasculariztion and to inhibit inflammatory-mediated processes as measured by endotoxin-induced nitric oxide release in vitro.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL279 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18311895 |
|||
Target ID: CHEMBL2634 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18311895 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. | 2008-03-27 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18311895
A 10 ul drop of (70 ug, 137 nM) is instilled per eye.
Route of Administration:
Topical
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
DTXSID20235791
Created by
admin on Mon Mar 31 18:45:19 GMT 2025 , Edited by admin on Mon Mar 31 18:45:19 GMT 2025
|
PRIMARY | |||
|
DB05075
Created by
admin on Mon Mar 31 18:45:19 GMT 2025 , Edited by admin on Mon Mar 31 18:45:19 GMT 2025
|
PRIMARY | |||
|
1VZO7A0J9S
Created by
admin on Mon Mar 31 18:45:19 GMT 2025 , Edited by admin on Mon Mar 31 18:45:19 GMT 2025
|
PRIMARY | |||
|
11973736
Created by
admin on Mon Mar 31 18:45:19 GMT 2025 , Edited by admin on Mon Mar 31 18:45:19 GMT 2025
|
PRIMARY | |||
|
867331-82-6
Created by
admin on Mon Mar 31 18:45:19 GMT 2025 , Edited by admin on Mon Mar 31 18:45:19 GMT 2025
|
PRIMARY |
SUBSTANCE RECORD