DERAZANTINIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C29H29FN4O
Molecular Weight	468.5652
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1

InChI

InChIKey=KPJDVVCDVBFRMU-AREMUKBSSA-N

InChI=1S/C29H29FN4O/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34)/t26-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C29H29FN4O
Molecular Weight	468.5652
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/28161661 | https://www.ncbi.nlm.nih.gov/pubmed/28240679 | https://clinicaltrials.gov/ct2/show/NCT01752920

Derazantinib (ARQ 087) is an investigational, oral, multi-kinase inhibitor designed to preferentially inhibit the FGFR family of kinases with demonstrated activity in FGFR2 genetic alterations, including fusions. In human cancers, FGFRs have been found to be dysregulated by multiple mechanisms, including aberrant expression, mutations, chromosomal rearrangements, and amplifications. FGFR dysregulation has been identified as a driver in a number of cancers, including iCCA, cholangiocarcinoma, bladder, endometrial, breast, gastric, lung and ovarian. Current scientific literature suggests FGFR alterations exist in anywhere from 5% to 40% of these cancers. Derazantinib is a potent FGFR inhibitor that shows strong anti-proliferative activity in cell lines harboring FGFR2 alterations. In clinical testing, the molecule has demonstrated activity in cancerous tumors harboring FGFR2 fusions in iCCA and bladder cancers.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Fibroblast growth factor receptor 2 25 Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808	Inhibitor 8504	1.8 nM [IC50]
Fibroblast growth factor receptor 1 46 Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808	Inhibitor 8504	4.5 nM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808	Inhibitor 8504	4.5 nM [IC50]
Fibroblast growth factor receptor 4 16 Target ID: CHEMBL3973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808	Inhibitor 8504	34.0 nM [IC50]
Tyrosine-protein kinase receptor RET 16 Target ID: CHEMBL2041 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808	Inhibitor 8504	3.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Solid tumors 147 Sources: https://clinicaltrials.gov/ct2/show/NCT01752920	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
164.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
963.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
1940.87 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20339.47 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
5 day EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5 day EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DERAZANTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY445236	https://www.001chemical.com/chem/search?q=DY445236
1PlusChem LLC	1P000L0X	https://www.1pchem.com/search?query=1P000L0X
AChemBlock	Q65421	http://www.achemblock.com/catalogsearch/result/?q=Q65421
AChemBlock	Q70199	http://www.achemblock.com/catalogsearch/result/?q=Q70199
AstaTech	43712	http://astatechinc.com/CPSResult.php?CRNO=43712
AstaTech	C71924	http://astatechinc.com/CPSResult.php?CRNO=C71924
BLD Pharm	BD768221	http://www.bldpharm.com/search/Search.html?keyword=BD768221
Chem Scene	CS-7922	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-7922
Chem Scene	CS-7923	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-7923
ChemShuttle	181939	https://www.chemshuttle.com/catalogsearch/result/?q=181939
ChemShuttle	185355	https://www.chemshuttle.com/catalogsearch/result/?q=185355
ChemShuttle	185356	https://www.chemshuttle.com/catalogsearch/result/?q=185356
eMolecules	275978271	https://orderbb.emolecules.com/search/#?query=275978271
eMolecules	303202913	https://orderbb.emolecules.com/search/#?query=303202913
eMolecules	89937112	https://orderbb.emolecules.com/search/#?query=89937112
MedChem Express	HY-19981	https://www.medchemexpress.com/search.html?q=HY-19981A&ft=&fa=&fp=
MedChem Express	HY-19981A	https://www.medchemexpress.com/search.html?q=HY-19981A&ft=&fa=&fp=
Molcore	MC445236	http://www.molcore.com/CatMC445236.html
Molnova	M10930	https://www.molnova.com/en/serch-list.html?keywords=M10930
MolPort	MolPort-046-418-485	https://www.molport.com/shop/molecule-link/MolPort-046-418-485
MolPort	MolPort-046-418-486	https://www.molport.com/shop/molecule-link/MolPort-046-418-486
MuseChem	I006437	https://www.musechem.com/product/I006437.html
MuseChem	I013145	https://www.musechem.com/product/I013145.html
Selleck Chemicals	S8609	http://www.selleckchem.com/search.html?searchDTO.searchParam=S8609
ShangHai Biochempartner	BCP29103	http://www.biochempartner.com/search_BCP29103
Toronto Research Chemicals	D281924	https://www.trc-canada.com/product-detail/?CatNum=D281924

PubMed

Title	Date	PubMed
Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.	2016	27627808

Patents

Sample Use Guides

In Vivo Use Guide

ARQ-087 orally at dose levels specified for their respective dose cohorts on a 28-day schedule. Dosing will begin at 25 mg every other day (QOD) and will escalate until the maximum tolerated dose (MTD)

Route of Administration: Oral

In Vitro Use Guide

NCI-H716 and SNU-16 cells were plated and incubated at 37°C overnight and subsequently treated with 0.1 μM or 1 μM of ARQ 087 for 24 or 72 hours. The cells were fixed and stained with Cycletest Plus Reagent kit (BD Biosciences, Franklin Lakes, NJ) according to the manufacturer’s instructions, and cell cycle profiles were analyzed using a FACS Calibur flow cytometer

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:12:05 GMT 2025` Edited by `admin` on `Mon Mar 31 20:12:05 GMT 2025`
Record UNII	N9B0H171MJ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

derazantinib [INN]

Preferred Name

English

DERAZANTINIB

Official Name

English

Derazantinib [WHO-DD]

Common Name

English

ARQ 087

Code

English

DERAZANTINIB [USAN]

Common Name

English

ARQ087

Code

English

BENZO(H)QUINAZOLIN-2-AMINE, 6-(2-FLUOROPHENYL)-5,6-DIHYDRO-N-(3-(2-((2-METHOXYETHYL)AMINO)ETHYL)PHENYL)-, (6R)-

Systematic Name

English

ARQ-087

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1967