Derazantinib, Inhibitor

Derazantinib

Cat. Num. AAA5764480

• Purity: 99.95%
• Synonyms: Derazantinib; ARQ-087; inhibitor

• Purity/Purification: 99.95%
• Form/Format: Solid. Powder

• Solubility: DMSO: 98mg/mL (209.15mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C29H29FN4O
• SMILES: COCCNCCc1cccc(Nc2ncc3C[C@@H](c4ccccc4F)c4ccccc4-c3n2)c1
• CAS Number: 1234356-69-4
• Cell Research: Cells are seeded at 3000-5000 cells per well with 130uL media in 96-well tissue culture-treated plates. The cells are incubated overnight and subsequently treated with 3-fold serial dilutions of Derazantinib starting at 100uM. The cells are returned to a 37 degree C humidified incubator for 72 hours. Cell proliferation is measured using the MTS assay [1].
• Kinase Assay: Derazantinib is titrated in DMSO utilizing a 3-fold dilution scheme and then diluted 10-fold further in deionized water for a final DMSO concentration of 10%. A volume (2.5 uL) of these dilutions or vehicle is added to each well of a reaction plate. FGFR1 or FGFR2 is added to assay buffer to each well in a volume of 17.5uL for a final concentration of 0.50 or 0.25nM, respectively. After a 30-minute pre-incubation period, ATP and substrate are added in assay buffer (5 uL) for final concentrations of 0-1,000uM ATP and 80nM biotinylated-PYK2, for a final reaction volume of 25 uL. The plates are incubated for 60 minutes at room temperature and then stopped in the dark by the addition of 10uL stop/detection mixture prepared in assay buffer containing EDTA [1].
• In Vitro: Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplification and fusions [1]. Most of the embryos exhibit abnormal external phenotype (81.3%) in Derazantinib-injected wings, possibly due to inhibition of proliferation of limb bud mesenchyme [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Derazantinib, inhibitor

Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5nM/1.8nM/4.5nM).

Product Categories/Family for Derazantinib, inhibitor

Angiogenesis; FGFR; Tyrosine Kinase/Adaptors

References

Hall TG, et al. Preclinical Activity of ARQ-087, a Novel Inhibitor Targeting FGFR Dysregulation. PLoS One. 2016 Sep 14;11(9):e0162594.
Hall TG, et al. Preclinical Activity of ARQ-087, a Novel Inhibitor Targeting FGFR Dysregulation. PLoS One. 2016 Sep 14;11(9):e0162594.
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.
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.