533063 VPS34 Inhibitor, SAR405

533063
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₂₁ClF₃N₅O

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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®
      Synonyms(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, Vacuolar Protein Sorting 34 Inhibitor, SAR405
      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.