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Derazantinib(ARQ-087) - 99%, high purity , Fibroblast growth factor receptor inhibitor, CAS No.1234356-69-4, Fibroblast growth factor receptor inhibitor

Moligand™
≥99%

CAS#: 1234356-69-4
Formula: C₂₉H₂₉FN₄O
Molecular Weight: 468.57
MDL number: MFCD30532770
PubChem CID: 46834118

Item Number

D302670

Grouped product items
SKU	Size	Availability	Price
D302670-1mg	1mg	In stock	$45.90
D302670-5mg	5mg	In stock	$187.90
D302670-25mg	25mg	In stock	$642.90

View related series

fibroblast growth factor receptor 1 Inhibitor fibroblast growth factor receptor 2 Inhibitor fibroblast growth factor receptor 3 Inhibitor

Basic Description

Synonyms	Derazantinib\|1234356-69-4\|ARQ-087\|ARQ087\|Derazantinib [USAN]\|ARQ 087\|Derazantinib (ARQ 087)\|N9B0H171MJ\|(6R)-6-(2-fluorophenyl)-N-[3-[2-(2-methoxyethylamino)ethyl]phenyl]-5,6-dihydrobenzo[h]quinazolin-2-amine\|Benzo[h]quinazolin-2-amine, 6-(2-fluorophenyl)-
Specifications & Purity	99%
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Fibroblast growth factor receptor inhibitor
Product Description	Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.

Associated Targets

FGFR1 Tclin Fibroblast growth factor receptor 1 1 Activities

Discover Target: FGFR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 1 Activities

Discover Target: FGFR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 1 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(6R)-6-(2-fluorophenyl)-N-[3-[2-(2-methoxyethylamino)ethyl]phenyl]-5,6-dihydrobenzo[h]quinazolin-2-amine
INCHI	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
InChi Key	KPJDVVCDVBFRMU-AREMUKBSSA-N
Canonical SMILES	COCCNCCC1=CC(=CC=C1)NC2=NC=C3CC(C4=CC=CC=C4C3=N2)C5=CC=CC=C5F
Isomeric SMILES	COCCNCCC1=CC(=CC=C1)NC2=NC=C3C[C@H](C4=CC=CC=C4C3=N2)C5=CC=CC=C5F
PubChem CID	46834118
Molecular Weight	468.57

CAS Registry No.

1234356-69-4

PubChem CID

46834118

Certificates

Certificate of Analysis(COA)

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3 results found

Lot Number	Certificate Type	Date	Item
I2126029	Certificate of Analysis	Jul 16, 2024	D302670
I2126030	Certificate of Analysis	Jul 16, 2024	D302670
I2126397	Certificate of Analysis	Jul 16, 2024	D302670

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

References

1. Hall TG, Yu Y, Eathiraj S, Wang Y, Savage RE, Lapierre JM, Schwartz B, Abbadessa G. (2016) Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.. PLoS ONE, 11 (9): (e0162594). [PMID:27627808]
2. Papadopoulos KP, El-Rayes BF, Tolcher AW, Patnaik A, Rasco DW, Harvey RD, LoRusso PM, Sachdev JC, Abbadessa G, Savage RE et al.. (2017) A Phase 1 study of ARQ 087, an oral pan-FGFR inhibitor in patients with advanced solid tumours.. Br J Cancer, 117 (11): (1592-1599). [PMID:28972963]

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