Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H14ClN3O2.ClH |
| Molecular Weight | 352.215 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC
InChI
InChIKey=WDJDYIUSDDVWKB-UHFFFAOYSA-N
InChI=1S/C16H14ClN3O2.ClH/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11;/h3-9H,1-2H3,(H,18,19,20);1H
| Molecular Formula | C16H14ClN3O2 |
| Molecular Weight | 315.754 |
| 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 |
AG1478 (also known as Tyrphostin AG 1478 ) is a selective EGFR inhibitor, which induced cell cycle arrest in G1 phase, is developed as potential drug for nasopharyngeal carcinoma treatment. In addition was shown, that AG1478 effectively blocked the leiomyoma cell growth and is unaffected by the presence of physiological concentrations of progesterone and estradiol. The growth-arresting properties of AG1478, unaffected by ovarian steroidal hormones, identify it as a potential lead agent for the non-surgical management of uterine leiomyomas. Also was investigated the action of the combination AG1478 in combination with HGF tyrosine kinase inhibitors on non-small cell lung cancer (NSCLC) cells, and was suggested, that these combinations of drugs could be potentially used for treatment of NSCLC.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| UV-Vis spectroscopy and solvatochromism of the tyrosine kinase inhibitor AG-1478. | 2016-07-05 |
|
| Epidermal growth factor receptor inhibitor AG1478 inhibits mucus hypersecretion in airway epithelium. | 2016-02-13 |
|
| Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. | 1996-09-01 |
Patents
Sample Use Guides
xenografted mice: treated with saline as placebo, 0.4 mg AG1478 i.p.
Route of Administration:
Intravenous
AG1478 (1-1000 nM) significantly inhibited both LPS-induced and TNF-α-induced secretion of MUC5AC and IL-8 from cultured NCI-H292 cells in a dose-dependent manner. The expression of MUC5AC and IL-8 messenger RNAs was also significantly inhibited. Intranasal instillation of AG1478 one hour after intranasal LPS instillation significantly inhibited LPS-induced goblet cell metaplasia, mucus production, and neutrophil infiltration in rat nasal epithelium, as did intraperitoneal injection of AG1478 one hour before LPS instillation.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Apr 01 23:35:33 GMT 2025
by
admin
on
Tue Apr 01 23:35:33 GMT 2025
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| Record UNII |
QP952C4RUW
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| Record Status |
Validated (UNII)
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| Record Version |
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3035187
Created by
admin on Tue Apr 01 23:35:33 GMT 2025 , Edited by admin on Tue Apr 01 23:35:33 GMT 2025
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QP952C4RUW
Created by
admin on Tue Apr 01 23:35:33 GMT 2025 , Edited by admin on Tue Apr 01 23:35:33 GMT 2025
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PARENT -> SALT/SOLVATE |
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