Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C25H20N6O |
| Molecular Weight | 420.4659 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CC(=N1)C2=C(N=C(CC3=CC(=CC=C3)C(N)=O)N2)C4=CC5=NC=CN=C5C=C4
InChI
InChIKey=RYKSGWSKILPDDY-UHFFFAOYSA-N
InChI=1S/C25H20N6O/c1-15-4-2-7-20(29-15)24-23(17-8-9-19-21(14-17)28-11-10-27-19)30-22(31-24)13-16-5-3-6-18(12-16)25(26)32/h2-12,14H,13H2,1H3,(H2,26,32)(H,30,31)
| Molecular Formula | C25H20N6O |
| Molecular Weight | 420.4659 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022989 | https://www.ncbi.nlm.nih.gov/pubmed/18951571 | https://www.ncbi.nlm.nih.gov/pubmed/24887560
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022989 | https://www.ncbi.nlm.nih.gov/pubmed/18951571 | https://www.ncbi.nlm.nih.gov/pubmed/24887560
IN-1130 as a potent small molecule inhibitor of TGF-β signaling pathway. IN-1130 is a highly selective small molecule ALK5 inhibitor with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. It is a suppressor of fibrogenic process of unilateral ureteral obstruction in rats underscoring the potential clinical benefits in the treatment of renal fibrosis. IN-1130 may potentially treat prostate cancer and breast cancer (preclinical investigation phase).
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4439 |
36.0 nM [IC50] | ||
Target ID: CHEMBL260 |
4.3 µM [IC50] | ||
Target ID: CHEMBL2007 |
7.8 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| IN-1130, a novel transforming growth factor-beta type I receptor kinase (activin receptor-like kinase 5) inhibitor, promotes regression of fibrotic plaque and corrects penile curvature in a rat model of Peyronie's disease. | 2009-05 |
|
| Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/activin receptor-like kinase-5, on prostate cancer cells. | 2008-12 |
|
| Identification of human cytochrome P450 enzymes involved in the metabolism of IN-1130, a novel activin receptor-like kinase-5 (ALK5) inhibitor. | 2008-05 |
|
| Pharmacokinetics and tissue distribution of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide; a novel ALK5 inhibitor and a potential anti-fibrosis drug. | 2008-03 |
Patents
Sample Use Guides
40 mg/kg in 100 ul saline 3 times per week for 3 weeks.
Route of Administration:
Intraperitoneal
| Substance Class |
Chemical
Created
by
admin
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Edited
Mon Mar 31 21:46:49 GMT 2025
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on
Mon Mar 31 21:46:49 GMT 2025
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| Record UNII |
KW4O83PQ97
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| Record Status |
Validated (UNII)
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