Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

676489 VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem

The VEGFR2 Kinase Inhibitor IV, also referenced under CAS 216661-57-3, controls the biological activity of VEGFR2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: KDR/Flk-1 Kinase Inhibitor IV, 3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine, Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XVIII, VEGFR1 Kinase Inhibitor II, VEGFR3 Kinase Inhibitor II, PDGFR Tyrosine Kinase Inhibitor IX

Primary Target: VEGFR-2 KDR/Flk-1
676489
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
216661-57-3C₁₇H₁₃N₃OS
Description
Overview

This product has been discontinued.





A 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, reversible, and ATP-competitive inhibitor of VEGFR-2 (KDR/Flk-1; IC50 = 19 nM). Displays ~2-fold greater selectivity for VEGFR-2 over PDGFRβ (IC50 = 34 nM) and 10-fold greater selectivity over VEGFR-1 (Flt-1) and VEGFR-3 (Flt-4; IC50 = 190 nM) tyrosine kinase activity. Does not inhibit FGFR-1 or Src kinase activity (IC50 > 1.9 µM). Shown to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC50 = 387 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.
Catalogue Number676489
Brand Family Calbiochem®
SynonymsKDR/Flk-1 Kinase Inhibitor IV, 3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine, Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XVIII, VEGFR1 Kinase Inhibitor II, VEGFR3 Kinase Inhibitor II, PDGFR Tyrosine Kinase Inhibitor IX
References
ReferencesCools, J., et al. 2004. Cancer Res. 64, 6385.
Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.
Product Information
CAS number216661-57-3
ATP CompetitiveY
FormYellow solid
Hill FormulaC₁₇H₁₃N₃OS
Chemical formulaC₁₇H₁₃N₃OS
ReversibleY
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetVEGFR-2 KDR/Flk-1
Primary Target IC<sub>50</sub>19 nM
Purity≥95% by HPLC
Physicochemical Information
Cell permeableN
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
676489 0

Documentation

VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

VEGFR2 Kinase Inhibitor IV - CAS 216661-57-3 - Calbiochem Certificates of Analysis

TitleLot Number
676489

References

Reference overview
Cools, J., et al. 2004. Cancer Res. 64, 6385.
Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-January-2010 RFH
SynonymsKDR/Flk-1 Kinase Inhibitor IV, 3-(3-Thienyl)-6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidine, Vascular Endothelial Growth FactorReceptor 2 Kinase Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XVIII, VEGFR1 Kinase Inhibitor II, VEGFR3 Kinase Inhibitor II, PDGFR Tyrosine Kinase Inhibitor IX
DescriptionA 3,6-diaryl substituted pyrazolopyrimidine that acts as a potent, reversible, and ATP-competitive inhibitor of vascular endothelial cell growth factor receptor-2 (VEGFR-2; KDR/Flk-1) (IC50 = 19 nM). Displays ~2-fold greater selectivity for VEGFR-2 compared to platelet derived growth factor receptor β (PDGFRβ) and 10-fold selectivity compared to VEGFR-1 (Flt-1) and VEGFR-3 (Flt-4). Does not inhibit FGFR-1 or Src kinase activity. Reported to inhibit VEGF-stimulated mitogenesis in human umbilical vein endothelial cells (IC50 = 387 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number216661-57-3
Chemical formulaC₁₇H₁₃N₃OS
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (5 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCools, J., et al. 2004. Cancer Res. 64, 6385.
Fraley, M.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 2767.