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Details

Stereochemistry ACHIRAL
Molecular Formula C29H29FN4O.2ClH
Molecular Weight 541.488
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DERAZANTINIB HYDROCHLORIDE

SMILES

COCCNCCc1cccc(c1)Nc2ncc3C[C@]([H])(c4ccccc4-c3n2)c5ccccc5F.Cl.Cl

InChI

InChIKey=OLDWOVJAXRWCGT-FBHGDYMESA-N
InChI=1S/C29H29FN4O.2ClH/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);2*1H/t26-;;/m1../s1

HIDE SMILES / InChI

Molecular Formula C29H29FN4O
Molecular Weight 468.5662
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: 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.

Approval Year

TargetsConditions

Conditions

PubMed

PubMed

TitleDatePubMed
Patents

Patents

Sample Use Guides

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
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 Sat Jun 26 06:35:37 UTC 2021
Edited
by admin
on Sat Jun 26 06:35:37 UTC 2021
Record UNII
U6B7J0L31Q
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DERAZANTINIB HYDROCHLORIDE
USAN  
Official Name English
BENZO(H)QUINAZOLIN-2-AMINE, 6-(2-FLUOROPHENYL)-5,6-DIHYDRO-N-(3-(2-((2-METHOXYETHYL)AMINO)ETHYL)PHENYL)-, HYDROCHLORIDE (1:2), (6R)-
Systematic Name English
ARQ-087 DIHYDROCHLORIDE
Code English
DERAZANTINIB HYDROCHLORIDE [USAN]
Common Name English
DERAZANTINIB DIHYDROCHLORIDE
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 497615
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
EU-Orphan Drug EU/3/16/1657
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
NCI_THESAURUS C1967
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
Code System Code Type Description
PUBCHEM
124081779
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
PRIMARY
CAS
1234352-08-9
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
NON-SPECIFIC STOICHIOMETRY
FDA UNII
U6B7J0L31Q
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
PRIMARY
CAS
1821329-75-2
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
PRIMARY
NCI_THESAURUS
C143047
Created by admin on Sat Jun 26 06:35:37 UTC 2021 , Edited by admin on Sat Jun 26 06:35:37 UTC 2021
PRIMARY
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