Details
Stereochemistry | ACHIRAL |
Molecular Formula | C33H30ClN5O3.ClH |
Molecular Weight | 616.537 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=C2N=C(NC3=CC=C(OCCN4CCCC4)C=C3)N=NC2=CC(=C1)C5=CC(OC(=O)C6=CC=CC=C6)=CC=C5Cl
InChI
InChIKey=VLWKPMDUDFMWBO-UHFFFAOYSA-N
InChI=1S/C33H30ClN5O3.ClH/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);1H
Molecular Formula | C33H30ClN5O3 |
Molecular Weight | 580.076 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
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Target ID: CHEMBL2634 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18311895 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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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 Mar 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
Substance Class |
Chemical
Created
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admin
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Sat Dec 16 08:06:29 GMT 2023
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Record UNII |
PFJ9GB4R1J
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Record Status |
Validated (UNII)
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