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428207 Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate

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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1188890-30-3C₂₅H₂₈N₆O₃ • H₂O
Description
Overview

This product has been discontinued.



A cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC50 = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC50 = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).
Catalogue Number428207
Brand Family Calbiochem®
Synonyms2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate
References
ReferencesSabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.
Product Information
CAS number1188890-30-3
FormOff-white solid
Hill FormulaC₂₅H₂₈N₆O₃ • H₂O
Chemical formulaC₂₅H₂₈N₆O₃ • H₂O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% 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 Regulatory Review
Storage +2°C to +8°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
Catalogue Number GTIN
428207 0

Documentation

Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem Certificates of Analysis

TitleLot Number
428207

References

Reference overview
Sabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.
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.

Revision25-May-2011 RFH
Synonyms2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate
DescriptionA cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC50 = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC50 = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1188890-30-3
Chemical formulaC₂₅H₂₈N₆O₃ • H₂O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (25 mg/ml)
Storage Protect from light
+2°C to +8°C
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.
Toxicity Regulatory Review
ReferencesSabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973.