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438194 LRRK2 Inhibitor II, CZC-25146 - Calbiochem

The LRRK2 Inhibitor II, CZC-25146 controls the biological activity of LRRK2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

LRRK2 Inhibitor II, CZC-25146 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(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

438194
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₂H₂₅FN₆O₄S•HCl

Products

Catalogue NumberPackaging Qty/Pack
438194-10MG Glass bottle 10 mg
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
Catalogue 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.