1821329-75-2

1821329-75-2 structure

Name: Derazantinib dihydrochloride
Chemical Name: ARQ-087 dihydrochloride
CAS Number: 1821329-75-2
Molecular Formula: C₂₉H₃₁Cl₂FN₄O
Molecular Weight: 541.487
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2018-06-13 04:30:03
Modify Date: 2024-01-12 12:42:12
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].

Name	ARQ-087 dihydrochloride
Synonyms	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

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.