Product Description: 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].
Applications: Cancer-Kinase/protease
Formula: C29H29FN4O
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: 1234356-69-4
Molecular Weight: 468.57
Compound Purity: 99.28
Research Area: Cancer
Solubility: DMSO : 25 mg/mL (ultrasonic)
Target: FGFR