505146 | FMS/KIT Dual Kinase Inhibitor, PLX647 - Calbiochem

505146
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₁H₁₇F₃N₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05146.0001
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          Glass bottle 10 mg
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          Description
          OverviewA 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®
          Synonymsc-Kit Inhibitor IV, 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, 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

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

          Revision27-September-2013 JSW
          Synonymsc-Kit Inhibitor IV, 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, 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 -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
          ReferencesZhang, C., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 5689.