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VEGFR Tyrosine Kinase Inhibitor IV

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号:676483-500UG

牌:Millipore 密理博

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Replacement Information

重要规格表

Empirical Formula CAS #
C₂₂H₁₉ClN₄O₅ • H₂O 475108-18-0
Description
Overview 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 Number 676483
Brand Family Calbiochem®
Synonyms Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, PDGFR Tyrosine Kinase Inhibitor XII, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V
References
References Nakamura, K., et al. 2006. Cancer Res. 66, 9134.
Product Information
CAS number 475108-18-0
ATP Competitive N
Form Pink solid
Hill Formula C₂₂H₁₉ClN₄O₅ • H₂O
Chemical formula C₂₂H₁₉ClN₄O₅ • H₂O
Reversible N
Structure formula Image Structure formula Image
Applications
Biological Information
Primary Target VEGFR
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 permeable Y
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 Instructions Following 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

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