LDN-211904,5MG,428201-5MGCN,Sigma

销售价: ¥ 2191.30 / 件
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订货号 0BV6334
品牌型号 Sigma 428201-5MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

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)
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)


技术参数 Specifications
Quality Segment100
assay≥99% (HPLC)
formsolid
potency79 nM IC50
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,protect from light
color off-white
solubilityDMSO: 50 mg/mL, clear, nearly colorless
shipped inambient
storage temp.2-8°C
SMILES stringO=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O
InChI1S/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 keyODBJGLKPAQMCJA-UHFFFAOYSA-N
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