ALOFANIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H15N3O6S
Molecular Weight	413.404
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC(=C(NS(=O)(=O)C2=CC(=CC=C2)C(O)=O)C=C1C3=CN=CC=C3)[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	413.404
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26597690 | https://adisinsight.springer.com/drugs/800043004 | https://www.ncbi.nlm.nih.gov/pubmed/27812884

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.

Originator

Approval Year

PubMed

Title	Date	PubMed
Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2.	2015 Nov	26597690
Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models.	2016 Jul	27136102

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

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). Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms.In a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibited FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibited the proliferation and migration of human and mouse endothelial cells (GI50 11-58 nmol/l).

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:27:03 GMT 2023` Edited by `admin` on `Sat Dec 16 11:27:03 GMT 2023`
Record UNII	LQX7RFK8MZ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ALOFANIB

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