| CAS NO: | 948557-43-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 439.53 |
|---|---|
| Formula | C26H21N3O2S |
| CAS No. | 948557-43-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 35 mg/mL (79.6 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 2% Cremophor EL, 2% N,N-dimethylacetamide: 30 mg/mL |
| Synonyms | Synonym: Tie2-inhibitor-5; Tie2 IN 5; Tie2IN5; Tie2 kinase inhibitor 5; Tie2-IN-5; Tie2 inhibitor 5; Compound 5; Chemical Name: 4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]pyridine InChi Key: SINQIEAULQKUPD-UHFFFAOYSA-N InChi Code: InChI=1S/C26H21N3O2S/c1-31-22-8-5-19-15-21(4-3-20(19)16-22)25-24(17-11-13-27-14-12-17)28-26(29-25)18-6-9-23(10-7-18)32(2)30/h3-16H,1-2H3,(H,28,29) SMILES Code: O=S(C1=CC=C(C2=NC(C3=CC=C4C=C(OC)C=CC4=C3)=C(C5=CC=NC=C5)N2)C=C1)C |
| In Vitro | In vitro activity: Tie2 kinase inhibitor exhibits a moderate inhibitory activity against Tie2 tyrosine kinase. Tie2 kinase inhibitor also shows moderate cellular activities with IC50 of 232 nM in HEL cells. Furthermore, Tie2 kinase inhibitor has a remarkable selectivity for Tie2 over p38 (IC50=50 μM) and a>10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β. Kinase Assay: Turned on an incubator shaker and adjusted temperature to 30 °C. Added 20 μL of 3× kinase buffer (final 20 mM Tris-HCl, pH 7, 100 mM NaCl, 12 mM MgCl2, 1 mM DTT) per well to the Flashplate. Added 20 μL of protein per well except for background. Added Tie2 Kinase Inhibitor, typically 1 ~ 2 μL in DMSO stocks. Added 20 μL of a mixture of gamma 33p-ATP and cold ATP (1:1 v/v) per well. Covered with transparent polyester film. Incubated at 30 °C for 2 hrs in shaker, washed five times. Read plate on TopCount or other counting instrument, and results were calculated as IC50 values using normal methods. Cell Assay: In HEL cells, Tie2 Kinase Inhibitor moderately suppressed the activity of Tie2 tyrosine kinase, with an IC50 value of 232 NM. |
|---|---|
| In Vivo | In a Matrigel mouse model of angiogenesis, Tie2 kinase inhibitor, at doses of 25 and 50 mg/kg (i.p., b.i.d), leads to a reduction of 41% and 70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor treatment results in a modest dose dependent delay in tumor growth. |
| Animal model | MOPC-315 plasmacytoma xenograft model. |
| Formulation & Dosage | Dissolved in 5% EtOH+5%cremophor+90% water.; 50 mg/kg; i.p. injection |
| References | Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60 |
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