VEGFR-3-IN-1

SKU: orb1744565

Description

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor (IC50 = 110.4 nM) that blocks the VEGFR3 signaling pathway. It demonstrates antitumor activity by suppressing the proliferation and migration of VEGF-C-stimulated HDLECs and breast cancer cells like MDA-MB-231 in vitro.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2756668-73-0
• MW: 616.1
• Purity: 99.95% (May vary between batches)
• Formula: C₂₉H₂₉ClF₃N₇OS
• SMILES: C(NC1=CC(C(F)(F)F)=C(Cl)C=C1)(=O)N2CCN(C3=C4C(SC(=C4)C5=CC=C(C=C5)N6CCN(C)CC6)=NC=N3)CC2
• Target: VEGFR
• Solubility: DMSO:1 mg/mL (1.62 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.62 mM)

Bioactivity

• Target IC50:
  VEGFR3:110.4 nM
• In Vivo:
  VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours.
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• In Vitro:
  VEGFR-3-IN-1 (50, 25 mg/kg; oral; once; nude mice) achieved the most potent tumor volume inhibition in nude mice, with an inhibition rate of 61.9%.The results of VEGFR-3-IN-1 (10 mg/kg; oral) post-treatment showed a maximal concentration (Cmax) of 420 ng/mL, an AUC0-t of 9219 ng-h /mL, AUC0-∞ of 12,304 ng-h/mL, and a half-life (t1/2) of 16 hours.
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Storage & Handling

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

Alternative Names

VEGFR3

Compound Identifiers

PubChem CID

156587562