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428201 LDN-211904 - Calbiochem

428201
Purchase on Sigma-Aldrich

Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical Formula
C₂₁H₂₁ClN₄O₅

Products

Numero di catalogoConfezionamento Qtà/conf
428201-5MG Bottiglia di vetro 5 mg
Description
OverviewA pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC50 of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.
Catalogue Number428201
Brand Family Calbiochem®
SynonymsEphB3 inhibitor, LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate
References
ReferencesQiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122
Product Information
FormOff-white solid
Hill FormulaC₂₁H₂₁ClN₄O₅
Chemical formulaC₂₁H₂₁ClN₄O₅
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetErythropoietin-producing hepatocellular carcinoma (Eph)
Primary Target IC<sub>50</sub>79 nM
Purity≥99% 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 +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
Transport Information
Supplemental Information
Specifications

Documentation

LDN-211904 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

LDN-211904 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
428201

Riferimenti bibliografici

Panoramica delle referenze
Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122
Scheda tecnica

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.

Revision09-July-2012 JSW
SynonymsEphB3 inhibitor, LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate
DescriptionA pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC50 of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.
FormOff-white solid
Chemical formulaC₂₁H₂₁ClN₄O₅
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml; clear, nearly colorless solution)
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 3 months at -20°C.
Toxicity Standard Handling
ReferencesQiao, L., et al. 2011, Bioorg. Med. Chem. Lett. 19, 6122