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TCS 7010 (Aurora A Inhibitor I; TCS-7010 ) is a novel, potent, and highly selective inhibitor of Aurora A kinase-AAK with potential antitumor activity. It inhibits Aurora A kinase with an IC50 of 3.4 nM in a cell-free assay and shows 1000-fold higher selectivity for Aurora A over Aurora B. TCS7010 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.
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Physicochemical Properties
| Molecular Formula |
C31H31CLFN7O2
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| Molecular Weight |
588.07
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| Exact Mass |
587.221
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| CAS # |
1158838-45-9
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| Related CAS # |
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| PubChem CID |
44139710
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.679
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| LogP |
4.39
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
42
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| Complexity |
862
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AKSIZPIFQAYJGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H31ClFN7O2/c1-2-39-15-17-40(18-16-39)28(41)19-21-7-11-24(12-8-21)36-31-34-20-26(33)29(38-31)35-23-13-9-22(10-14-23)30(42)37-27-6-4-3-5-25(27)32/h3-14,20H,2,15-19H2,1H3,(H,37,42)(H2,34,35,36,38)
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| Chemical Name |
N-(2-Chlorophenyl)-4-[[2-[[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]phenyl]amino]-5-fluoro-4-pyrimidinyl]amino]-benzamide
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| Synonyms |
| TC S 7010; TCS 7010; TC-S7010 |
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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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Biological Activity
| ln Vitro |
TCS7010 is an incredibly specific inhibitor of Aurora A. Without the added burden of simultaneously blocking Aurora B, TCS7010 is a helpful tool chemical for examining the cellular function of Aurora A kinases[1].
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| ln Vivo |
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| Animal Protocol |
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| References |
[1]. Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E, Liang J, Moffat J, Phillips G, Pulk R, Rawson TE, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhu BY, Cochran AG.A class of 2,4-bisanilinopy.
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| Additional Infomation |
N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide is a member of benzamides.
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Solubility Data
| Solubility (In Vitro) |
| DMSO: 118 mg/mL (200.6 mM) | | Water:<1 mg/mL | | Ethanol:<1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.
(Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions |
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1 mg |
5 mg |
10 mg |
| 1 mM |
1.7005 mL |
8.5024 mL |
17.0048 mL |
| 5 mM |
0.3401 mL |
1.7005 mL |
3.4010 mL |
| 10 mM |
0.1700 mL |
0.8502 mL |
1.7005 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. |
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