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TAS-119 (VIC 1911; TAS-2104) is a novel, potent and orally bioavailable inhibitor of the serine/threonine protein kinase aurora A with potential antimitotic and antineoplastic activities.
| ln Vitro |
In a variety of human cancer cell lines, including paclitaxel-resistant cells, TAS-119 increases the antiproliferative effects of paclitaxel [1]. Three taxanes (paclitaxel, docetaxel, and cabazitaxel) that suppress cell proliferation in HeLa cells are dose-dependently enhanced by TAS-119 (30-300 nM). When comparing normal diploid fibroblasts to tumor cells, TAS-119 largely causes mitotic accumulation in the latter [1].
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| ln Vivo |
TAS-119 (5-30 mg/kg; oral; twice daily on day 1 and twice daily on day 2) therapy promotes phosphorylated histone H3 (pHH3) in HeLa-luc xenograft nude mice[1] .
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| Animal Protocol |
Animal/Disease Models: Nude mice were injected with HeLa-luc cells [1].
Doses: 5 mg/kg, 10 mg/kg, 30 mg/kg. Route of Administration: oral administration; injection administration. twice (two times) daily on day 1 and twice (two times) daily on day 2 Experimental Results: In nude mice with HeLa-luc xenografts, all doses induced pHH3. |
| References | |
| Additional Infomation |
Aurora A Kinase Inhibitor VIC-1911 is an orally bioavailable inhibitor of the serine/threonine protein kinase aurora A, with potential antimitotic and antineoplastic activities. Upon intravenous administration, aurora A kinase inhibitor VIC-1911 binds to and inhibits aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, inhibition of cell division and the induction of apoptosis in cells overexpressing aurora A kinase. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis; it plays an essential role in the regulation of spindle assembly. Aurora kinase A is overexpressed in a wide variety of cancers.
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| Molecular Formula |
C23H22CL2FN5O3
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|---|---|
| Molecular Weight |
506.3569
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| Exact Mass |
505.108
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| CAS # |
1453099-83-6
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| PubChem CID |
71696703
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| Appearance |
White to off-white solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
741
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(=C([H])C([H])=C([H])C=1C(N1C([H])([H])C([H])([H])C(C(=O)O[H])(C([H])([H])C2C([H])=C([H])C(=C(N([H])C3C([H])=C(C([H])([H])[H])N([H])N=3)N=2)F)C([H])([H])C1([H])[H])=O)Cl
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| InChi Key |
PLAVWQHGBMTMFR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22Cl2FN5O3/c1-13-11-18(30-29-13)28-20-17(26)6-5-14(27-20)12-23(22(33)34)7-9-31(10-8-23)21(32)15-3-2-4-16(24)19(15)25/h2-6,11H,7-10,12H2,1H3,(H,33,34)(H2,27,28,29,30)
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| Chemical Name |
1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridin-2-yl]methyl]piperidine-4-carboxylic acid
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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 |
| 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) |
DMSO : ~50 mg/mL (~98.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.11 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 20.8 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: 2.08 mg/mL (4.11 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9749 mL | 9.8744 mL | 19.7488 mL | |
| 5 mM | 0.3950 mL | 1.9749 mL | 3.9498 mL | |
| 10 mM | 0.1975 mL | 0.9874 mL | 1.9749 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.
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