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438194 LRRK2 Inhibitor II, CZC-25146 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₂₅FN₆O₄S•HCl

Pricing & Availability

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438194-10MG
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      Glass bottle 10 mg
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      Description
      OverviewAn orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50 = 4.76 and 6.87 nM for hr-wt-LRRK2 and G2019S-LRRK2 mutant, respectively) with selectivity over PLK4, GAK, TNK1, CAMKK2, and PIP4K2C (IC50 < 300 nM) in a 185-kinase panel. Does neither exert cytotoxicity nor block neuronal development of human or rat cortical neurons at 1 µM. Shown to prevent GS-LRRK2-induced neuronal injury (EC50 ~4 nM) and G2019S- or R1441C-LRRK2-mediated neuronal death in both rat and human cortical neurons (EC50 ~ 100 nM). Even though exhibits favorable pharmacokinetic profile and metabolic stability, and yet suffers from limited blood brain barrier penetration (~4%).
      Catalogue Number438194
      Brand Family Calbiochem®
      SynonymsN-(2-(5-Fluoro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl, N-(2-(2-(2-Methoxy-4-morpholinophenylamino)-5-fluoropyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl
      References
      ReferencesRamsden, N., et al. 2011. ACS Chem. Biol. 6, 1021.
      Product Information
      FormGreyish to off-white powder
      Hill FormulaC₂₂H₂₅FN₆O₄S•HCl
      Chemical formulaC₂₂H₂₅FN₆O₄S•HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      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 +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 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
      438194-10MG 04055977187038

      Documentation

      LRRK2 Inhibitor II, CZC-25146 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      LRRK2 Inhibitor II, CZC-25146 - Calbiochem Certificates of Analysis

      TitleLot Number
      438194

      References

      Reference overview
      Ramsden, N., et al. 2011. ACS Chem. Biol. 6, 1021.
      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.

      Revision20-July-2012 JSW
      SynonymsN-(2-(5-Fluoro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl, N-(2-(2-(2-Methoxy-4-morpholinophenylamino)-5-fluoropyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl
      DescriptionAn orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50 = 4.76 and 6.87 nM for hr-wt-LRRK2 and G2019S-LRRK2 mutant, respectively) with selectivity over PLK4, GAK, TNK1, CAMKK2, and PIP4K2C (IC50 < 300 nM) in a 185-kinase panel. Does neither exert cytotoxicity nor block neuronal development of human or rat cortical neurons at 1 µM. Shown to prevent GS-LRRK2-induced neuronal injury (EC50 ~4 nM) and G2019S- or R1441C-LRRK2-mediated neuronal death in both rat and human cortical neurons (EC50 ~ 100 nM). Even though exhibits favorable pharmacokinetic profile and metabolic stability, and yet suffers from limited blood brain barrier penetration (~4%).
      FormGreyish to off-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₅FN₆O₄S•HCl
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml) or H₂O (1 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesRamsden, N., et al. 2011. ACS Chem. Biol. 6, 1021.