Derazantinib
Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM) . Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models[1][2].
Product Specifications
CAS Number
1234356-69-4
Product Name Alternative
ARQ-087
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
FGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Derazantinib.html
Purity
99.19
Solubility
DMSO : 25 mg/mL (ultrasonic)
Smiles
COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1
Molecular Formula
C29H29FN4O
Molecular Weight
468.57
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
Frequently Asked Questions
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