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Derazantinib

Catalog No. TQ0228   CAS 1234356-69-4
Synonyms: ARQ-087

Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM).

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Derazantinib Chemical Structure
Derazantinib, CAS 1234356-69-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
2 mg In stock $ 91.00
5 mg In stock $ 155.00
10 mg In stock $ 253.00
25 mg In stock $ 538.00
50 mg In stock $ 778.00
100 mg In stock $ 1,090.00
1 mL * 10 mM (in DMSO) In stock $ 158.00
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Purity: 99.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM).
Targets&IC50 FGFR2:1.8 nM, FGFR1:4.5 nM, FGFR3:4.5 nM
In vitro In cells, Derazantinib effectively inhibits FGFR2 auto-phosphorylation and the activity of proteins downstream in the FGFR pathway (FRS2α, AKT, ERK), showcasing its anti-proliferative effects on cell lines affected by FGFR dysregulation due to amplifications, fusions, and mutations. Studies reveal a clear correlation between Derazantinib's ability to induce G1 cell cycle arrest and promote apoptosis in cell lines with elevated FGFR2 protein. Additionally, Derazantinib counteracts FGF2-mediated growth arrest with an EC50 of approximately 100 nM, maintaining safety at concentrations up to 500 nM and significantly inhibiting FGF2 effects within a 70-500 nM range. Beyond its influence on cell proliferation, Derazantinib prevents FGF-mediated deterioration of the extracellular matrix and premature chondrocyte senescence, supporting chondrocyte differentiation in tibia cultures. Its inhibitory action is specific to FGFR1-4, distinguishing Derazantinib from other receptor tyrosine kinases inhibitors in cell-free kinase assays, and extends to FGFR1 and FGFR2 mutants linked to craniosynostoses.
In vivo Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplification and fusions [1]. Most of the embryos exhibit abnormal external phenotype (81.3%) in Derazantinib-injected wings, possibly due to inhibition of proliferation of limb bud mesenchyme [2].
Kinase Assay Derazantinib is titrated in DMSO utilizing a 3-fold dilution scheme and then diluted 10-fold further in deionized water for a final DMSO concentration of 10%. A volume (2.5 μL) of these dilutions or vehicle is added to each well of a reaction plate. FGFR1 or FGFR2 is added to assay buffer to each well in a volume of 17.5 μL for a final concentration of 0.50 or 0.25 nM, respectively. After a 30-minute pre-incubation period, ATP and substrate are added in assay buffer (5 μL) for final concentrations of 0-1,000 μM ATP and 80 nM biotinylated-PYK2, for a final reaction volume of 25 μL. The plates are incubated for 60 minutes at room temperature and then stopped in the dark by the addition of 10 μL stop/detection mixture prepared in assay buffer containing EDTA [1].
Cell Research Cells are seeded at 3000-5000 cells per well with 130 μL media in 96-well tissue culture-treated plates. The cells are incubated overnight and subsequently treated with 3-fold serial dilutions of Derazantinib starting at 100 μM. The cells are returned to a 37°C humidified incubator for 72 hours. Cell proliferation is measured using the MTS assay [1].
Animal Research Female NCr nu/nu mice (SNU-16) or CB17 SCID mice (NCI-H716) with well established (400 mg) subcutaneous tumors are given a single oral dose of Derazantinib or vehicle control. Plasma and tumor samples are collected 4 hours post single dose. Derazantinib is administered orally. The dosing volume for all groups is 10 mL/kg or 0.1 mL/10 g body weight [1].
Synonyms ARQ-087
Molecular Weight 468.57
Formula C29H29FN4O
CAS No. 1234356-69-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 98 mg/mL (209.15 mM)

TargetMolReferences and Literature

1. Hall TG, et al. Preclinical Activity of ARQ-087, a Novel Inhibitor Targeting FGFR Dysregulation. PLoS One. 2016 Sep 14;11(9):e0162594. 2. Balek L, et al. ARQ-087 inhibits FGFR signaling and rescues aberrant cell proliferation and differentiation in experimental models of craniosynostoses and chondrodysplasias caused by activating mutations in FGFR1, FGFR2 and FGFR3. Bone. 2017 Dec;105:57-66.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Liver Cancer Compound Library ReFRAME Related Library Reprogramming Compound Library Anti-Cancer Compound Library Anti-Fibrosis Compound Library Bioactive Compounds Library Max

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Keywords

Derazantinib 1234356-69-4 Angiogenesis Tyrosine Kinase/Adaptors FGFR ARQ-087 ARQ087 Fibroblast growth factor receptor inhibit ARQ 087 Inhibitor inhibitor

 

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