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428205 Lck Inhibitor - CAS 213743-31-8 - Calbiochem

428205
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
213743-31-8C₂₃H₂₂N₄O

Products

Catalogue NumberPackaging Qty/Pack
428205-1MG Plastic ampoule 1 mg
Description
OverviewA cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells) and in vivo (ED50 = 4 mg/kg in mice, ip.)
Catalogue Number428205
Brand Family Calbiochem®
Synonyms4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
References
ReferencesBurchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
Product Information
CAS number213743-31-8
ATP CompetitiveY
FormWhite solid
Hill FormulaC₂₃H₂₂N₄O
Chemical formulaC₂₃H₂₂N₄O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetLck₆₄₋₅₀₉ Y³⁹⁴
Primary Target IC<sub>50</sub>At5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk
Purity≥95% 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 Ambient Temperature Only
Toxicity Harmful
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 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Lck Inhibitor - CAS 213743-31-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Lck Inhibitor - CAS 213743-31-8 - Calbiochem Certificates of Analysis

TitleLot Number
428205

References

Reference overview
Burchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
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.

Revision12-January-2010 RFH
Synonyms4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
DescriptionA cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells) and in vivo (ED50 = 4 mg/kg in mice, ip.)
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number213743-31-8
Chemical formulaC₂₃H₂₂N₄O
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (17 mg/ml)
Storage +2°C to +8°C
Protect from light
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 Harmful
ReferencesBurchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.