Lucitanib

SKU: orb1308358

Description

Lucitanib (E-3810) is a potent and selective small molecule inhibitor targeting vascular endothelial growth factor receptors (VEGFR1/2/3) and fibroblast growth factor receptors (FGFR1/2). It has demonstrated anti-angiogenic and anti-tumor activity in preclinical studies, supporting its investigation in oncology research, particularly for cancers driven by these signaling pathways.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1058137-23-7
• MW: 443.49
• Purity: 97.33% (May vary between batches)
• Formula: C₂₆H₂₅N₃O₄
• SMILES: CNC(=O)c1cccc2cc(Oc3ccnc4cc(OCC5(N)CC5)c(OC)cc34)ccc12
• Target: VEGFR,FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.51 mM);DMSO:25 mg/mL (56.37 mM)

Bioactivity

• Target IC50:
  FGFR1:17.5 nM|VEGFR3:10 nM|FGFR2:82.5 nM|VEGFR1:7 nM|VEGFR2:25 nM
• In Vivo:
  Lucitanib (20 mg/kg; 7 consecutive days; p.o.) treatment, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed. The activity of Lucitanib given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib , with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib at a rate similar to control tumors. Lucitanib displays a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas). It has dose-dependent inhibition of tumor growth.
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• In Vitro:
  Lucitanib potently inhibits FGFR2 activity (Ki<0.05 μM), follows by PDGFRα activity (Ki=0.11 μM) and it also potently inhibits VEGF and bFGF-stimulated HUVEC proliferation (IC50: 40 and 50 nM, respectively), which consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation. Lucitanib (E-3810) also inhibits CSF-1R (IC50: 5 nM).The Ki values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E3810, E-3810, E 3810, Lucitanib, inhibit, Inhibitor, FGFR, FGFR2, FGFR1, Fibroblast growth factor receptor, Vascular endothelial growth factor receptor, VEGFR3, VEGFR, VEGFR1, VEGFR2

Compound Identifiers

PubChem CID

25031915