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533063 VPS34 Inhibitor, SAR405

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₂₁ClF₃N₅O

Products

Catalog NumberPackaging Qty/Pack
5.33063.0001 Glass bottle 5 mg
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
Global Trade Item Number
Catalog Number GTIN
5.33063.0001 04055977282061

Documentation

VPS34 Inhibitor, SAR405 SDS

Title

Safety Data Sheet (SDS) 

VPS34 Inhibitor, SAR405 Certificates of Analysis

TitleLot Number
533063

References

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