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Purity: ≥98%
Tie2 kinase inhibitor, optimized from SB-203580, is a reversible, selective and ATP-competitive Tie2 inhibitor with potential antitumor activity. It has a 200-fold selectivity over p38 towards Tie2. A xenograft model of MOPC-315 plasmacytoma demonstrated strong antitumor activity when treated with a Tie2 kinase inhibitor.
| Targets |
Tie2 (IC50 = 250 nM)
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| ln Vitro |
Tie2 kinase inhibitors have a moderately strong inhibitory effect on Tie2 tyrosine kinase. With an IC50 of 232 nM in HEL cells, the Tie2 kinase inhibitor likewise exhibits moderate cellular activity. Moreover, Tie2 kinase inhibitor exhibits >10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β and a remarkable selectivity for Tie2 over p38 (IC50=50 μM).[1]
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| ln Vivo |
Tie2 kinase inhibitors at doses of 25 and 50 mg/kg (i.p., b.i.d.) reduce angiogenesis in a Matrigel mouse model of angiogenesis by 41% and 70%, respectively. Treatment with a Tie2 kinase inhibitor slows tumor growth in a dose-dependent manner in a MOPC-315 plasmacytoma xenograft model.[1]
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| Enzyme Assay |
Turned on an incubator shaker and adjusted temperature to 30 °C. To the Flashplate, 20 μL of 3× kinase buffer (final 20 mM Tris-HCl, pH 7, 100 mM NaCl, 12 mM MgCl2, 1 mM DTT) was added per well. except for background, 20 μL of protein were added to each well. Additional Tie2 Kinase Inhibitor, usually 1–2 μL in DMSO stocks. For each well, 20 μL of a 1:1 v/v combination of cold ATP and gamma 33p-ATP was added. Film made of translucent polyester was used to cover. five washes and two hours of incubation at 30 °C in a shaker. IC50 values were computed using standard methods after the plate was read on TopCount or another counting device.
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| Cell Assay |
Tie2 Kinase Inhibitor had an IC50 value of 232 NM and moderately inhibited the activity of Tie2 tyrosine kinase in HEL cells.
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| Animal Protocol |
MOPC-315 plasmacytoma xenograft model.
≤50 mg Administered via i.p. |
| References |
| Molecular Formula |
C26H21N3O2S
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|---|---|---|
| Molecular Weight |
439.53
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| Exact Mass |
439.14
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| Elemental Analysis |
C, 71.05; H, 4.82; N, 9.56; O, 7.28; S, 7.29
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| CAS # |
948557-43-5
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
COC1=CC2=C(C=C1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)S(=O)C)C5=CC=NC=C5
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| InChi Key |
SINQIEAULQKUPD-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
4-[4-(6-methoxynaphthalen-2-yl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine
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| Synonyms |
Tie2-inhibitor-5; Tie2IN5; Tie2-IN-5; Tie2 kinase inhibitor 5; Tie2 inhibitor 5; Compound 5; Tie2 IN 5
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.79 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.79 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2% Cremophor EL, 2% N,N-dimethylacetamide: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2752 mL | 11.3758 mL | 22.7516 mL | |
| 5 mM | 0.4550 mL | 2.2752 mL | 4.5503 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2752 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60. |
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60. |
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60. |
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