428201
LDN-211904
LDN-211904 modulates the biological activity of EphB3 receptor tyrosine kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate, EphB3 inhibitor, LDN-211904
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关于此项目
经验公式（希尔记法）:
C21H21ClN4O5
化学文摘社编号:
分子量:
444.87
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C19H19ClN4O.C2H2O4/c20-15-3-1-2-4-16(15)23-19(25)17-11-22-18-6-5-14(12-24(17)18)13-7-9-21-10-8-13;3-1(4)2(5)6/h1-6,11-13,21H,7-10H2,(H,23,25);(H,3,4)(H,5,6)
InChI key
ODBJGLKPAQMCJA-UHFFFAOYSA-N
SMILES string
O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O
assay
≥99% (HPLC)
form
solid
potency
79 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 50 mg/mL, clear, nearly colorless
shipped in
ambient
Quality Level
General description
A 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Erythropoietin-producing hepatocellular carcinoma (Eph)
Erythropoietin-producing hepatocellular carcinoma (Eph)
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett.19, 6122
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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