Derazantinib Inhibitor

Name: Derazantinib Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5764480
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5764480

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). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Derazantinib, Inhibitor

Full Product Name

Derazantinib

Product Synonym Names

ARQ-087

Form/Format

Solid. Powder

Purity/Purification

99.95%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

468.57

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].

Product Categories/Family for Derazantinib, inhibitor

Angiogenesis; FGFR; Tyrosine Kinase/Adaptors

Product References and Citations for Derazantinib, inhibitor

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.

Other Notes

Small volumes of Derazantinib, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Derazantinib purchase

MBS5764480 is an inhibitor targeting Derazantinib.