Vatalanib hydrochloride

SKU: orb2565080

Description

Vatalanib hydrochloride (PTK787 hydrochloride) is a potent, orally active VEGF receptor tyrosine kinase inhibitor. It has demonstrated efficacy in reducing cortical Aβ plaque burden in 5xFAD Alzheimer's disease mouse models and is also widely used in oncology research to study angiogenesis in vitro and in vivo.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 212141-52-1
• MW: 383.27
• Purity: 99.70%
• Formula: C₂₀H₁₆Cl₂N₄
• SMILES: Cl.ClC1=CC=C(C=C1)NC2=NN=C(C=3C=CC=CC23)CC=4C=CN=CC4
• Target: VEGFR,Apoptosis
• Solubility: DMSO:50 mg/mL (130.46 mM)

Bioactivity

• Target IC50:
  c-Kit:730 nM|Flk:270 nM|PDGFRβ:580 nM|HUVECs:7.1 nM
• In Vivo:
  Vatalanib hydrochloride administered orally once daily (25-100 mg/kg) dose-dependently inhibited angiogenic responses induced by VEGF and PDGF in growth factor implantation models and tumor cell-driven angiogenesis models. Vatalanib hydrochloride also effectively inhibited the growth and metastasis of several human cancers in nude mice at the same dose range, with no significant effect on circulating blood cells or bone marrow leukocytes.
• In Vitro:
  Vatalanib hydrochloride also inhibited Flk, c-Kit, and PDGFRβ with IC50s of 270 nM, 730 nM, and 580 nM, respectively.Vatalanib hydrochloride exerted its anti-proliferative effect in HUVECs by inhibiting VEGF-induced thymidine doping (IC50 of 7.1 nM) and dose-dependently inhibited VEGF-induced endothelial cell survival and migration over a similar dose range, with no significant cytotoxic or antiproliferative effects on cells not expressing VEGF receptors. Vatalanib hydrochloride significantly inhibited the growth of hepatocellular carcinoma cells and enhanced IFN/5-FU-induced apoptosis by elevating the level of Bax protein and reducing the expression of Bcl-xL and Bcl-2 proteins.

Storage & Handling

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

Alternative Names

CGP797870 hydrochloride, CGP-797870 hydrochloride, Apoptosis, ZK222584 hydrochloride, ZK-222584 hydrochloride, PTK787 hydrochloride, PTK 787 hydrochloride, VEGFR2

Compound Identifiers

PubChem CID

9886292