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1821329-75-2

1821329-75-2 structure
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
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.  

Molecular Formula C29H31Cl2FN4O
Molecular Weight 541.487
Exact Mass 540.185913