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Details

Stereochemistry ACHIRAL
Molecular Formula C26H22FN7O
Molecular Weight 467.4976
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of AG-13958

SMILES

CN1N=C(C)C=C1C(=O)NC2=C(F)C=CC(NC3=CC=C4C(NN=C4\C=C\C5=CC=CC=N5)=C3)=C2

InChI

InChIKey=JXSVVZKPEDIRTN-DHZHZOJOSA-N
InChI=1S/C26H22FN7O/c1-16-13-25(34(2)33-16)26(35)30-24-15-19(7-10-21(24)27)29-18-6-9-20-22(31-32-23(20)14-18)11-8-17-5-3-4-12-28-17/h3-15,29H,1-2H3,(H,30,35)(H,31,32)/b11-8+

HIDE SMILES / InChI

Molecular Formula C26H22FN7O
Molecular Weight 467.4976
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Pfizer developed AG-013958, also known as AG-13958 for treatment of age-related macular degeneration (AMD). As a VEGFR tyrosine kinase inhibitor, AG13958 was targeted to FLT/TYK receptor inhibition.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minimal
PubMed

PubMed

TitleDatePubMed

Sample Use Guides

Unknown
Route of Administration: Other
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:55:55 GMT 2023
Edited
by admin
on Fri Dec 15 15:55:55 GMT 2023
Record UNII
BK72RP7F7D
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AG-13958
Common Name English
AG 13958
Code English
1H-PYRAZOLE-5-CARBOXAMIDE, N-(2-FLUORO-5-((3-((1E)-2-(2-PYRIDINYL)ETHENYL)-1H-INDAZOL-6-YL)AMINO)PHENYL)-1,3-DIMETHYL-
Systematic Name English
Code System Code Type Description
ChEMBL
CHEMBL3545335
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY
PUBCHEM
9934283
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY
FDA UNII
BK72RP7F7D
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY
EPA CompTox
DTXSID20953842
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY
MANUFACTURER PRODUCT INFORMATION
N-(2-FLUORO-5-((3-((1E)-2-(2-PYRIDINYL)ETHENYL)-1H-INDAZOL-6-YL)AMINO)PHENYL)-1,3-DIMETHYL-1H-PYRAZOLE-5-CARBOXAMIDE
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY SYN-1004, CAS 319460-94-1: AG13958 is a VEGF inhibitor that was clinical development by Pfizer in 2006-07 for treatment of age-related macular degeneration (AMD). The drug displays low water solubility and so far in trials delivery has been difficult needing direct injection to be truly effective and it varied by the species used because of species specific differences in eye circulation and vascularization. As a VEGF inhibitor AG13958 was targeted to FLT/TYK receptor inhibition.
CAS
319460-94-1
Created by admin on Fri Dec 15 15:55:55 GMT 2023 , Edited by admin on Fri Dec 15 15:55:55 GMT 2023
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
SOLVATE->ANHYDROUS
Related Record Type Details
ACTIVE MOIETY
Class: Eye disorder therapy; Mechanism of Action: Angiogenesis inhibitor, Vascular endothelial growth factor A inhibitor; Highest Development Phase: Discontinued for Age-related macular degeneration; Most Recent Events: 11 Mar 2008 Discontinued - Phase-I/II for Age-related macular degeneration in Australia (Ophthalmic), 11 Mar 2008 Discontinued - Phase-I/II for Age-related macular degeneration in United Kingdom (Ophthalmic), 11 Mar 2008 Discontinued - Phase-I/II for Age-related macular degeneration in Netherlands (Ophthalmic)