533063 VPS34 Inhibitor, SAR405

533063
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₂₁ClF₃N₅O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33063.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable pyrimido[1,2-a]pyrimidin-6(2H)-one derivative that acts as a potent, selective, and ATP competitive inhibitor of vacuolar protein sorting 34 kinase activity (Vps34; Kd = 1.5 nM, IC50 = 1.2 nM in a biochemical assay, and IC50 = 27 nM in a cell based assay). Does not affect the activity of over 200 other protein kinases including class I and II PI 3 kinases and mTOR (~ 10 µM). However, it displays a weak inhibitory activity against SMG1 at higher concentrations (IC50 = 1 µM). Does not affect the Akt phosphorylation even at higher concentrations (~10 µM), Shown to affect the late endosome-lysosome compartment formation and block the formation of autophagosomes in starved HeLa and H1299 cells (~ 1 µM). Acts synergistically with everolimus to block the proliferation of ACHN and 786-O renal tumor cells.
          Catalogue Number533063
          Brand Family Calbiochem®
          SynonymsVacuolar Protein Sorting 34 Inhibitor, SAR405, (S)-1-((5-chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one
          References
          ReferencesRonan, B., et al. 2014. Nat. Chem. Biol. 10, 1013.
          Product Information
          FormOff-white powder
          Hill FormulaC₁₉H₂₁ClF₃N₅O
          ReversibleY
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetVPS34
          Primary Target K<sub>i</sub>1.5 nM, IC₅₀
          Purity≥96% 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 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

          VPS34 Inhibitor, SAR405 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Ronan, B., et al. 2014. Nat. Chem. Biol. 10, 1013.