EOC317

SKU: orb1302956

Description

EOC317 (ACTB-1003) is an orally bioavailable small molecule inhibitor targeting FGFR1, VEGFR2, and Tie-2 kinases with IC50 values of 6, 2, and 4 nM, respectively. It is utilized in preclinical research to investigate angiogenesis and tumor growth in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 939805-30-8
• MW: 591.53
• Purity: 99.26% (May vary between batches)
• Formula: C₂₇H₂₆F₅N₇O₃
• SMILES: COCc1c(CN2CCOCC2)n2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)c(F)c1
• Target: FGFR,Tie-2,VEGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (4.23 mM);DMSO:55 mg/mL (92.98 mM)

Bioactivity

• Target IC50:
  VEGFR2:2 nM|FGFR1:6 nM|Tie2:4 nM
• In Vivo:
  ACTB-1003 inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. The combination ACTB-1003 with 5-FU or paclitaxel not diminish the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model.
• In Vitro:
  ACTB-1003 targets cancer mutations via FGFR inhibition FGFR1 (IC50: 6 nM), angiogenesis through inhibition of VEGFR2 (2 nM) and Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). In cell lines with FGFR genetic alterations - OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1, ACTB-1003 can markedly and dose-dependently inhibit tumor growth. OPM2 cells harbor the FGFR3 t (4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACTB 1003, ACTB1003, ACTB-1003, EOC 317, EOC317, EOC-317, Fibroblast growth factor receptor, FGFR, FGFR1, Inhibitor, inhibit, VEGFR2, VEGFR, Vascular endothelial growth factor receptor, Tie2, Tie-2

Compound Identifiers

PubChem CID

23653175