Vatalanib (PTK787) 2HCl

Catalog No.S1101 Synonyms: ZK 222584 (cpg-79787) 2HCl

Vatalanib (PTK787) 2HCl Chemical Structure

Molecular Weight(MW): 419.73

Vatalanib (PTK787) 2HCl is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.

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Cited by 10 Publications

3 Customer Reviews

  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Vatalanib (PTK787) 2HCl purchased from Selleck.

    Mechanisms of VEGF-activated Ca2 entry. All data were from HUVECs. a, Mean 100 ng/mL VEGF-evoked Ca2 entry in the presence of 100 nmol/L sorafenib (n/N3/40), 10 nmol/L vatalanib (n/N=3/24), or 10 mol/L U73122 (n/N=3/24) normalized to their matched controls. b and c, eYFP-STIM1 (green) before (control) (b) and after exposure to 100 ng/mL VEGF (c). d, Summary data for 100 ng/mL VEGF-evoked transient and sustained Ca2 signals after transfection with STIM1.si or sc.si (n/N3/64). e, Example merged image of a cell labeled with anti-VEGFR2 antibody (green), anti-Orai1 antibody (red), and the nuclear counter stain, DAPI (blue).

    Circ Res 2011 108, 1190-1198. Vatalanib (PTK787) 2HCl purchased from Selleck.

  • (Aa-Ja) A single row of BTs on the intact fin and stump after 6-14 dot with PTK787 and 4-12 dot with T. Small BTs appear in the fin regenerate after 8 dot with PTK787 and 6 dot with T (Da,Ea). A small BT cluster appears on the regenerate after 14 dot with PTK787 and 12 dot with T (Ga,Ha). (Ab-Jb) After 4 dot with T, BTs develop on the regenerate, stump and intact fin and continue to grow from 6-12 dot. (Jb) After 12 dot, the blood vessel network of T-treated females is similar to that of males. (Ac-Jc) PTK787-treated females do not possess BTs. (Aa-Ja,Ac-Jc) Neo-angiogenesis and regenerative outgrowth are inhibited in all PTK787-treated females. (Ad-Jd) System water controls regenerate normally and do not grow BTs. B.F., brightfield. Fli, fli1a:EGFP (green). KR21 (red) outlines the BTs. White vertical lines indicate the amputation plane. Scale bar: 100 um.

    Development 2013 140, 4323-34. Vatalanib (PTK787) 2HCl purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Vatalanib (PTK787) 2HCl is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
Targets
VEGFR2/KDR [1]
(Cell-free assay)		 VEGFR1/FLT1 [1]
(Cell-free assay)		 VEGFR2/Flk1 [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)		 VEGFR3/FLT4 [1]
(Cell-free assay)
37 nM 77 nM 270 nM 580 nM 660 nM
In vitro

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, 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. [1] 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. [2]

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). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes. [1]

Protocol

Kinase Assay:[1]
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VEGF Receptor Tyrosine Kinase Assays :

The in vitro kinase assays are performed in 96-well plates as a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-Sepharose. γ-[33P]ATP is used as the phosphate donor, and poly-(Glu:Tyr 4:1) peptide is used as the acceptor. Recombinant GST-fusion proteins are diluted in 20 mM Tris·HCl (pH 7.5) containing 1–3 mM MnCl2, 3–10 mM MgCl2, 0.25 mg/mL polyethylene glycol 20000, and 1 mM DTT, according to their specific activity. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1–3 mM MnCl2, 3–10 mM MgCl2, 3–8 μg/mL poly-(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT, and 0.2 μCi[γ-33P]ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 minutes at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Using a 96-well filter system, half the volume (20 μL) is transferred onto a Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively in 0.5% H3PO4 and then soaked in ethanol. After drying, Microscint cocktail is added, and scintillation counting is performed. IC50s for PTK787/ZK 222584 or SU5416 in these as well as all assays described below are calculated by linear regression analysis of the percentage inhibition.
Cell Research:[1]
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  • Cell lines: HUVECs
  • Concentrations: 0-10 μM
  • Incubation Time: 48 hours
  • Method: 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)
Animal Research:[1]
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  • Animal Models: A431 epithelial carcinoma, Ls174T colon carcinoma, HT-29 colon carcinoma, PC-3 prostate carcinoma, DU145 prostate carcinoma, and CWR-22 prostate carcinoma cells are injected s.c. into the nude mice.
  • Formulation: Vatalanib is dissolved in distilled water containing 5% DMSO and 1% Tween 80.
  • Dosages: 25-100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (202.51 mM)
Water 10 mg/mL (23.82 mM)
Ethanol 6 mg/mL (14.29 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 419.73
Formula

C20H15ClN4.2HCl
CAS No. 212141-51-0
Storage powder
in solvent
Synonyms ZK 222584 (cpg-79787) 2HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00390000 Active not recruiting Unspecified Adult Solid Tumor Protocol Specific Mayo Clinic|National Cancer Institute (NCI) January 2007 Phase 1
NCT00390000 Active not recruiting Unspecified Adult Solid Tumor Protocol Specific Mayo Clinic|National Cancer Institute (NCI) January 2007 Phase 1
NCT00615160 Suspended Melanoma University of Schleswig-Holstein December 2006 Phase 1|Phase 2
NCT00615160 Suspended Melanoma University of Schleswig-Holstein December 2006 Phase 1|Phase 2
NCT00385853 Completed Glioblastoma Massachusetts General Hospital|Dana-Farber Cancer Institute|Novartis September 2006 Phase 1
NCT00385853 Completed Glioblastoma Massachusetts General Hospital|Dana-Farber Cancer Institute|Novartis September 2006 Phase 1

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VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

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  • Most Potent VEGFR Inhibitor

    Axitinib : VEGFR1, VEGFR2, VEGFR3, IC50=0.1 nM, 0.2 nM, 0.1-0.3 nM.

  • FDA-approved VEGFR Inhibitor

    Axitinib : Approved by FDA for Renal Cell Carcinoma.

  • Classic VEGFR Inhibitor

    Dovitinib (TKI-258, CHIR-258) : Multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.

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  • Regorafenib (BAY 73-4506)

    Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.

  • Axitinib

    Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

    Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).

  • Cabozantinib (XL184, BMS-907351)

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  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID