Vatalanib dihydrochloride

SKU: orb1300525

Description

Vatalanib dihydrochloride

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 212141-51-0
• MW: 419.73
• Purity: 100.00%
• Formula: C₂₀H₁₅ClN₄·2HCl
• SMILES: Cl.Cl.Clc1ccc(Nc2nnc(Cc3ccncc3)c3ccccc23)cc1
• Target: PDGFR,Apoptosis,VEGFR
• Solubility: H2O:10 mg/mL (23.82 mM);DMSO:79 mg/mL (188.22 mM);Ethanol:6 mg/mL (14.29 mM)

Bioactivity

• Target IC50:
  VEGFR3/FLT4:660 nM|VEGFR2/Flk1:270 nM|VEGFR1/FLT1:77 nM|VEGFR2/KDR:37 nM|PDGFRβ:580 nM
• In Vivo:
  Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). Within this dose range, Vatalanib also inhibits growth and metastases of various human carcinomas in nude mice without significantly affecting circulating blood cells or bone marrow leukocytes.
• In Vitro:
  Vatalanib inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Moreover, Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.
• Cell Research:
  As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation is used. Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin and then incubated at 37 °C and 5% CO2 in growth medium. After 24 hours, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of PTK787/ZK 222584. As a control, wells without growth factor are also included. After 24 hours of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 hours before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′5,5′-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm. (Only for Reference)

Storage & Handling

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

Alternative Names

inhibit, Inhibitor, CGP-79787 dihydrochloride, CGP797870, CGP-797870, CGP797870 Dihydrochloride, CGP-797870 dihydrochloride, CGP-797870 Dihydrochloride, CGP79787, CGP-79787, CGP79787 Dihydrochloride, CGP-79787 Dihydrochloride, CGP 79787, CGP 79787 Dihydrochloride, CGP 797870, CGP 797870 Dihydrochloride, Apoptosis, ZK222584, ZK-222584, ZK222584 Dihydrochloride, ZK-222584 dihydrochloride, ZK-222584 Dihydrochloride, ZK 222584, ZK 222584 Dihydrochloride, PTK 787, PTK 787 Dihydrochloride, PTK787, PTK-787, PTK787 Dihydrochloride, PTK787 dihydrochloride, PTK-787 Dihydrochloride, PDGFRβ, Vatalanib, Vatalanib (PTK787), Vatalanib (PTK787) 2HCl, Vatalanib 2HCl, Vatalanib dihydrochloride, Vatalanib Dihydrochloride, Vascular endothelial growth factor receptor, VEGFR, VEGFR1/FLT1, VEGFR3/FLT4, VEGFR2/Flk1, VEGFR2/KDR

Compound Identifiers

PubChem CID

22386467