- 商品介绍
- 规格参数
- 包装参数
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)
| Quality Segment | 100 |
| 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 |
| storage temp. | 2-8°C |
| SMILES string | O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O |
| 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 |
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