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676483 VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII

Primary Target: VEGFR
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
475108-18-0C₂₂H₁₉ClN₄O₅ • H₂O
Description
Overview

This product has been discontinued.



A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC50 = 30, 6.5, and 15 nM for VEGFR-1,-2,and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC50 = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.
Catalogue Number676483
Brand Family Calbiochem®
SynonymsN-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII
References
ReferencesNakamura, K., et al. 2006. Cancer Res. 66, 9134.
Product Information
CAS number475108-18-0
ATP CompetitiveN
FormPink solid
Hill FormulaC₂₂H₁₉ClN₄O₅ • H₂O
Chemical formulaC₂₂H₁₉ClN₄O₅ • H₂O
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetVEGFR
Primary Target IC<sub>50</sub>30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively; 24, 40, 49, 78, and 78 nM for EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2, respectively
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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
676483 0

Documentation

VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem Certificates of Analysis

TitleLot Number
676483

References

Reference overview
Nakamura, K., et al. 2006. Cancer Res. 66, 9134.
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.

Revision19-April-2011 RFH
SynonymsN-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII
DescriptionA cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC50 = 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC50 = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.
FormPink solid
Intert gas (Yes/No) Packaged under inert gas
CAS number475108-18-0
Chemical formulaC₂₂H₁₉ClN₄O₅ • H₂O
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 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
ReferencesNakamura, K., et al. 2006. Cancer Res. 66, 9134.