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Products Details
Product Description
– Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models[1][2].
Web ID
– HY-19981B
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C29H31Cl2FN4O
References
– [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.
CAS Number
– 1821329-75-2
Molecular Weight
– 541.49
SMILES
– COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1.Cl.Cl
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– EGFR
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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