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505146 FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: CDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647

Primary Target: FMS
505146
  
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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₁H₁₇F₃N₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16 nM, respectively) by targeting the kinases in their inactive DGF-out conformation, while being less effective against Flt3, KDR/VEGFR2, CDC2L6/CDK11/CDK19, NTRK3/TrkC, DDR2, CDK8/cyclin C (IC50 = 91, 130, 350, 620, 700, and 710 nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel study (IC50 >1 µM). Shown to effectively inhibit cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 from 20 to 250 nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 from 92 to 380 nM). Exhibits in vivo efficacy in several murine inflammation models (20 to 80 mg/kg b.i.d.; p.o.) and in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30 mg/kg b.i.d.; p.o.).
      Catalogue Number505146
      Brand Family Calbiochem®
      SynonymsCDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647
      References
      ReferencesZhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.
      Product Information
      FormOff-white powder
      Hill FormulaC₂₁H₁₇F₃N₄
      Chemical formulaC₂₁H₁₇F₃N₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetFMS
      Secondary targetKIT
      Purity≥98% 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 -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
      Global Trade Item Number
      Bestellnummer GTIN
      505146 0

      Documentation

      FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Zhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.

      Broschüre

      Titel
      New Products Flyer- Feb 2014 - Vol 1
      Datenblatt

      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.

      Revision27-September-2013 JSW
      SynonymsCDC2L6/CDK11/CDK19 Inhibitor, CDK8 Inhibitor, cFMS Inhibitor V, CSF-1 Receptor Inhibitor V, CSF1R Inhibitor V, DDR2 Inhibitor II, Flt-3 Inhibitor VIII, IL-34 Receptor Inhibitor V, NTRK3/TrkC Inhibitor, VEGFR Tyrosine Kinase Inhibitor XXXVI, VEGFR2 Tyrosine Kinase Inhibitor XXXIV, c-Kit Inhibitor IV, PLX-647
      DescriptionA cell-permeable and bio-available azaindolylmethylpyridamine derivative that acts as a potent inhibitor against FMS and KIT (IC50 = 28 and 16 nM, respectively) by targeting and locking these two PDGF family receptor kinases in their inactive DGF-out conformation, while being less effective against Flt3, KDR/VEGFR2, CDC2L6/CDK11/CDK19, NTRK3/TrkC, DDR2, CDK8/cyclin C (IC50 = 91, 130, 350, 620, 700, and 710 nM, respectively) and exhibiting much reduced or little potency toward other kinases in a 400-kinase panel selectivity study (IC50 >1 µM). Shown to effectively inhibit CSF-1-induced (with RANKL as co-stimulator) osteoclast differentiation (IC50 = 170 nM), cellular FLT3-ITD, FMS, KIT phosphorylations (IC50 ranges from 20 to 250 nM), as well as FLT3-ITD-, FMS-, KIT-dependent proliferations (IC50 ranges from 92 to 380 nM), while being less effective against KDR- or wt FLT3-dependent proliferations (IC50 ranges from 1.6 to 5 µM). Orally available in rats (AUC0-∞ (h·µg/mL)/Cmax (µg/mL) = 6.4/0.63 and 46.35/3.72 post 10 mg/kg and 40 mg/kg oral dosage, respectively) and mice (AUC0-∞ (h·µg/mL)/Cmax (µg/mL) = 8.51/1.67 and 53.3/7.78 post 10 mg/kg and 40 mg/kg oral dosage, respectively) and is reported to exhibit in vivo efficacy in preventing rat MRMT-1 breast carcinoma bone metastases-caused osteolysis (30 mg/kg b.i.d.) as well as in blocking inflammation responses in several murine models, including UUO- (unilateral ureter obstruction) induced kidney inflammation (40 mg/kg b.i.d.), collagen-induced arthritis (20 to 80 mg/kg b.i.d.), LPS-induced serum IL-6 & TNF-α release (single 40 mg/kg oral dose 4.25 h before LPS), and mast cell activation-induced anaphylaxis (single 80 mg/kg oral dose 2 h before antigen stimulation).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₁₇F₃N₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesZhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.