TAK-593

SKU: orb1219200

Description

TAK-593 is an effective VEGFR and PDGFR family inhibitor (IC50s: 3.2, 0.95, 1.1, 4.3, and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα, and PDFGRβ, respectively).

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1005780-62-0
• MW: 445.47
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₃N₇O₃
• SMILES: O=C(C1=CC(C)=NN1C)NC2=CC(OC3=NN4C(C=C3)=NC(NC(C5CC5)=O)=C4)=CC=C2C
• Target: VEGFR
• Solubility: DMSO:45 mg/mL (101.02 mM)

Bioactivity

• In Vivo:
  TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50 = 3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50 = 4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50 = 10 nM) and Ret (IC50 = 18 nM) kinases. TAK-593 potently inhibits VEGF-and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts.
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• In Vitro:
  TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50 = 3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50 = 4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50 = 10 nM) and Ret (IC50 = 18 nM) kinases. TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

VEGFR