Derazantinib

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].

Product Specifications

CAS Number

[1234356-69-4]

Product Name Alternative

ARQ-087

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Derazantinib.html

Purity

99.19

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1

Molecular Formula

C29H29FN4O

Molecular Weight

468.57

Precautions

H302, H315, H319, H335

References & Citations

[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.