All AbMole products are for research use only, cannot be used for human consumption.
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.
| 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 |
| Molecular Weight | 468.57 |
| Formula | C29H29FN4O |
| CAS Number | 1234356-69-4 |
| Solubility (25°C) | DMSO 84 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FGFR Products |
|---|
| AZD4547
AZD4547 (Fexagratinib) is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively. |
| BGJ398 (Infigratinib)
BGJ398 (Infigratinib) is a potent and selective FGFR kinase inhibitor with IC50 values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| PD173074
PD173074 is a selective FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. |
| SSR128129E
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs. |
| LY2874455
LY2874455 is a novel and potent FGF/FGFR inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
