(Z)-Orantinib

SKU: orb1908974

Description

(Z)-Orantinib (SU6668) is a potent, orally bioavailable multi-kinase inhibitor targeting VEGFR2, PDGFRβ, and FGFR1. It demonstrates significant anti-angiogenic and anti-tumor activity in both cellular assays and in vivo models, making it a valuable research tool for studying tumor microenvironment and angiogenesis mechanisms.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 210644-62-5
• MW: 310.35
• Formula: C₁₈H₁₈N₂O₃
• SMILES: C(=C\1/C=2C(NC1=O)=CC=CC2)\C3=C(C)C(CCC(O)=O)=C(C)N3
• Target: Others
• Solubility: DMSO:40 mg/mL (128.89 mM)

Bioactivity

• Target IC50:
  FLK1/KDR:2.1 μM|FGFR1:1.2 μM|PDGFRβ:0.008 μM
• In Vivo:
  (Z)-Orantinib (4-200 mg/kg, orally administered for 21 days) demonstrated dose-dependent inhibitory effects on the growth of A431 tumors in nude mice . (Z)-Orantinib (75 mg/kg, administered intraperitoneally for 22 days) demonstrated significant inhibition of tumor angiogenesis and vascular formation in mice . (Z)-Orantinib (200 mg/kg, orally administered for 11-27 days) significantly induced regression of established large A431 parazacco spilurus subsp. spilurus xenograft tumors in nude mice .
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• In Vitro:
  (Z)-Orantinib (5-15 minutes) inhibits Flk-1 transphosphorylation, FGFR1 transphosphorylation, and PDGFR autophosphorylation, with Ki values of 2.1 μM, 1.2 μM, and 0.008 μM, respectively . (Z)-Orantinib (0.03-10 μM, 60 minutes) suppresses the increase in KDR tyrosine phosphorylation levels induced by VEGF in HUVECs . (Z)-Orantinib shows dose-dependent inhibitory effects on the mitogenic activity of VEGF- and FGF-induced HUVECs, with IC50 values of 0.34 μM and 9.6 μM, respectively .
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Storage & Handling

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

Alternative Names

(Z)-SU6668, (Z)-SU-6668, (Z)-TSU68, (Z)-TSU-68, (Z) Orantinib, (Z)Orantinib, Orantinib

Compound Identifiers

PubChem CID

5329099