Millipore Sigma Vibrant Logo

521238 PDGFRβ/RAF Kinase Inhibitor - Calbiochem

521238
View Pricing & Availability

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₁₆F₃N₇OS

Pricing & Availability

Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
521238-10MG
Retrieving availability...
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service

      Glass bottle 10 mg
      Retrieving price...
      Price could not be retrieved
      Minimum Quantity is a multiple of
      Maximum Quantity is
      Upon Order Completion More Information
      You Saved ()
       
      Request Pricing
      Description
      OverviewAn orally bioavailable amino-triazole compound that is shown to bind to the inactive conformations of both PDGFRβ and Raf kinases (allosteric, Type II inh), and acts as a potent inhibitor of Flt3, Kit, PDGFRα and PDGFRβ (Kd = 52, 170, 300 and 520 nM, respectively) with selectivity over B-Raf, p38α, FGFR2 and VEGFR2 (Kd > 10 µM) in a multi-kinase panel. Completely blocks the phosphorylations of MEK-1/2 S217/S221, ERK-1/2 T202/Y204 in FGF-stimulated HUVECs, PDGFRβ in PDGF-BB-stimulated VSMCs, ERK-1/2 T202/Y204 in 1205Lu-B Raf V600E cells, and C-Raf S338 at 10 µM. Reduces FGF-induced angiogenesis in mouse Matrigel model (50 mg/kg, i.p., bid) and selectively induces apoptosis in the endothelium; further, suppresses orthotopic renal cell carcinoma growth in mice (100 mg/kg, p.o., qd).
      Catalogue Number521238
      Brand Family Calbiochem®
      SynonymsPDGFR Tyrosine Kinase Inhibitor XXII, 6-(4-(5-(3-(Trifluoromethyl)phenylamino)-4 H-1,2,4-triazol-3-yl)phenoxy)-2-(methylthio)pyrimidin-4-amine
      References
      ReferencesMurphy, E.A., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 4299.
      Product Information
      FormBeige solid
      Hill FormulaC₂₀H₁₆F₃N₇OS
      Chemical formulaC₂₀H₁₆F₃N₇OS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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

      Documentation

      PDGFRβ/RAF Kinase Inhibitor - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PDGFRβ/RAF Kinase Inhibitor - Calbiochem Certificates of Analysis

      TitleLot Number
      521238

      References

      Reference overview
      Murphy, E.A., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 4299.
      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.

      Revision09-July-2012 JSW
      SynonymsPDGFR Tyrosine Kinase Inhibitor XXII, 6-(4-(5-(3-(Trifluoromethyl)phenylamino)-4 H-1,2,4-triazol-3-yl)phenoxy)-2-(methylthio)pyrimidin-4-amine
      DescriptionAn orally bioavailable amino-triazole compound that is shown to bind to the inactive conformations of both PDGFRβ and Raf kinases (allosteric, Type II inh), and acts as a potent inhibitor of Flt3, Kit, PDGFRα and PDGFRβ (Kd = 52, 170, 300 and 520 nM, respectively) with selectivity over B-Raf, p38α, FGFR2 and VEGFR2 (Kd > 10 µM) in a multi-kinase panel. Completely blocks the phosphorylations of MEK-1/2 S217/S221, ERK-1/2 T202/Y204 in FGF-stimulated HUVECs, PDGFRβ in PDGF-BB-stimulated VSMCs, ERK-1/2 T202/Y204 in 1205Lu-B Raf V600E cells, and C-Raf S338 at 10 µM. Reduces FGF-induced angiogenesis in mouse Matrigel model (50 mg/kg, i.p., bid) and selectively induces apoptosis in the endothelium; further, suppresses orthotopic renal cell carcinoma growth in mice (100 mg/kg, p.o., qd).
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₆F₃N₇OS
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesMurphy, E.A., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 4299.