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533063 VPS34 Inhibitor, SAR405 - CAS 1523406-39-4 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1523406-39-4C₁₉H₂₁ClF₃N₅O

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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
      CAS number1523406-39-4
      FormOff-white powder
      Hill FormulaC₁₉H₂₁ClF₃N₅O
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetVPS34
      Primary Target K<sub>i</sub>1.5 nM, IC₅₀
      Purity≥96% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5330630001 04055977282061