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Derazantinib dihydrochloride

Names

[ CAS No. ]:
1821329-75-2

[ Name ]:
Derazantinib dihydrochloride

[Synonym ]:
Benzo[h]quinazolin-2-amine, 6-(2-fluorophenyl)-5,6-dihydro-N-[3-[2-[(2-methoxyethyl)amino]ethyl]phenyl]-, (6R)-, hydrochloride (1:2)
(6R)-6-(2-Fluorophenyl)-N-(3-{2-[(2-methoxyethyl)amino]ethyl}phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride
U6B7J0L31Q

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM[1]


[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C29H31Cl2FN4O

[ Molecular Weight ]:
541.487

[ Exact Mass ]:
540.185913

Related Compounds