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Vatalanib (PTK-787; ZK222584; CGP79787) 2HCl

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Vatalanib (PTK-787; ZK222584; CGP79787) 2HCl
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Cat #: V0515 CAS #: 212141-51-0 Purity ≥ 98%

Description: Vatalanib (PTK787 or ZK-222584, cpg-79787 2HCl) 2HCl is a novel, potent and orally bioavailable inhibitor of VEGFR2/KDR with potential anticancer activity.

References: Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8

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Molecular Weight (MW)419.73
Molecular FormulaC20H15ClN4.2HCl
CAS No.212141-51-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 85 mg/mL (202.5 mM)r
Water: 10 mg/mL (23.8 mM)r
Ethanol: 6 mg/mL (14.3 mM)
SMILES CodeClC1=CC=C(NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4)C=C1.[H]Cl.[H]Cl
SynonymsZK 222584 (cpg-79787) 2HCl; ZK 222584; ZK222584; ZK-222584; PTK787; PTK 787; CGP 79787; CGP-797870; ZK-232934; PTK-787; ZK 232934; ZK232934; CGP79787D; PTK787/ZK 222584; CGP-7978.
ProtocolIn VitroVatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. 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.
In VivoVatalanib 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.3825 mL11.9124 mL23.8248 mL47.6497 mL
5mM0.4765 mL2.3825 mL4.7650 mL9.5299 mL
10mM0.2382 mL1.1912 mL2.3825 mL4.7650 mL
20mM0.1191 mL0.5956 mL1.1912 mL2.3825 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.