U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C19H15N3O6S
Molecular Weight 413.4057
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ALOFANIB

SMILES

Cc1cc(c(cc1-c2cccnc2)NS(=O)(=O)c3cccc(c3)C(=O)O)N(=O)=O

InChI

InChIKey=QUQGQIASFYWKAB-UHFFFAOYSA-N
InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24)

HIDE SMILES / InChI

Molecular Formula C19H15N3O6S
Molecular Weight 413.4057
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Russian Pharmaceutical Technologies is developing alofanib, a first in class, allosteric inhibitor of fibroblast growth factor receptor type 2 (FGFR2) for the treatment of tumours expressing FGFR2, including ovarian cancer, colorectal cancer and lung cancer. Alofanib is a potential allosteric inhibitor of FGFR2 used in oncology. Alofanib has potent effects on ovarian cancer growth in preclinical studies.The inhibitor blocks the extracellular part of the receptor and prevents its binding with the ligand. Alofanib suppressed proliferation of endothelial cells, their migration activity, and ability to form vessellike structures in vitro and significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo. The results indicate that Alofanib can inhibit angiogenesis.

Approval Year

PubMed

PubMed

TitleDatePubMed
Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2.
2015 Nov
Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models.
2016 Jul

Sample Use Guides

Mice: Daily intravenous regimen of alofanib (total maximum dose per week was 350 mg/kg) demonstrated significant effect (inhibiting growth by 80 % and by 53 % in comparison with vehicle and chemotherapy group alone, respectively
Route of Administration: Intravenous
Alofanib is an allosteric inhibitor of FGFR2 and significantly inhibited bFGF-induced proliferation of HUVEC cells (IC50 value of 11 nM) and suppressed proliferation of SVEC-4-10 cells (IC50 value of 58 nM).
Substance Class Chemical
Created
by admin
on Sat Jun 26 04:38:12 UTC 2021
Edited
by admin
on Sat Jun 26 04:38:12 UTC 2021
Record UNII
LQX7RFK8MZ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ALOFANIB
INN   WHO-DD  
INN  
Official Name English
ALOFANIB [INN]
Common Name English
ALOFANIB [WHO-DD]
Common Name English
BENZOIC ACID, 3-(((4-METHYL-2-NITRO-5-(3-PYRIDINYL)PHENYL)AMINO)SULFONYL)-
Systematic Name English
Code System Code Type Description
PUBCHEM
86280646
Created by admin on Sat Jun 26 04:38:12 UTC 2021 , Edited by admin on Sat Jun 26 04:38:12 UTC 2021
PRIMARY
INN
10171
Created by admin on Sat Jun 26 04:38:12 UTC 2021 , Edited by admin on Sat Jun 26 04:38:12 UTC 2021
PRIMARY
NCI_THESAURUS
C170744
Created by admin on Sat Jun 26 04:38:12 UTC 2021 , Edited by admin on Sat Jun 26 04:38:12 UTC 2021
PRIMARY
CAS
1612888-66-0
Created by admin on Sat Jun 26 04:38:12 UTC 2021 , Edited by admin on Sat Jun 26 04:38:12 UTC 2021
PRIMARY
FDA UNII
LQX7RFK8MZ
Created by admin on Sat Jun 26 04:38:12 UTC 2021 , Edited by admin on Sat Jun 26 04:38:12 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY