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ARQ-087

Cat. No. M6158
ARQ-087 Structure
Synonym:

Derazantinib

Size Price Availability Quantity
1mg USD 120  USD120 In stock
5mg USD 300  USD300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: In cells, inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) was evident by the response to ARQ 087 treatment. Cell proliferation studies demonstrated ARQ 087 has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein showed a positive relationship between ARQ 087 induced G1 cell cycle arrest and subsequent induction of apoptosis.

In vivo: ARQ 087 was effective at inhibiting tumor growth in vivo in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions. ARQ 087 is currently being studied in a phase 1/2 clinical trial that includes a sub cohort for intrahepatic cholangiocarcinoma patients with confirmed FGFR2 gene fusions.

Protocol
Cell Experiment
Cell lines COS-1 cells
Preparation method Cells were seeded at 3000–5000 cells per well with 130 μL media in 96-well tissue culture treated plates. The cells were incubated overnight and subsequently treated with 3-fold serial dilutions of ARQ 087 starting at 100 μM. The cells were returned to a 37°C humidified incubator for 72 hours.
Concentrations 100 μM
Incubation time 72 h
Animal Experiment
Animal models female NCr nu/nu mice (SNU-16) or CB17 SCID mice (NCI-H716)
Formulation DMA: cremophor EL: propylene glycol: 0.2 M acetate buffer, pH 5 (10:10:30:50)
Dosages 10 mL/kg or 0.1 mL/10 g
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 468.57
Formula C29H29FN4O
CAS Number 1234356-69-4
Purity >99%
Solubility DMSO 84 mg/mL
Storage at -20°C
References

[1] Balek L, et al. Bone. 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.

[2] Hall TG, et al. PLoS One. Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.

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Keywords: ARQ-087, Derazantinib supplier, FGFR, inhibitors

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