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Purity: ≥98%
TAK-901 (TAK901) is a novel and potent inhibitor of Aurora A/B kinases with potential antitumor activity. It inhibits Aurora A/B with IC50s of 21 nM and 15 nM, respectively, and shows little/no activity against JAK2, c-Src or Abl. TAK-901 displayed potent in vitro antiproliferative activity and high in vivo antitumor efficacy by binding to and inhibiting the activity of Aurora B, leading to a decrease in the proliferation of tumor cells that overexpress Aurora B.
| ln Vitro |
TAK-901 lowers cellular histone H3 phosphorylation and causes polyploidy in accordance with Aurora B suppression. It also shows time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. TAK-901, with effective concentration values ranging from 40 to 500 nM, suppresses cell proliferation in a variety of human cancer cell lines. Many kinases are inhibited when a large panel of kinases is examined in biochemical experiments. TAK-901, however, only weakly inhibits a few kinases in intact cells, such as FLT3 and FGFR2, aside from Aurora B [1].
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| ln Vivo |
TAK-901 shows strong action against many human solid tumor types in mouse xenografts, and it completely resolves the A2780 form of ovarian cancer. Additionally, TAK-901 showed strong efficacy against a number of leukemia models. TAK-901 produces pharmacologic effects that are correlated with its retention in tumor tissue and consistent with suppression of Aurora B[1].
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| References |
[1]. Farrell P, et al. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor. Mol Cancer Ther. 2013 Apr;12(4):460-70
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| Molecular Formula |
C28H32N4O3S
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| Molecular Weight |
504.64
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| CAS # |
934541-31-8
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| Related CAS # |
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| SMILES |
O=C(NC1CCN(CC1)C)C2=C(C3=C(C4=CC(C)=CN=C4N3)C(C5=CC=CC(S(=O)(CC)=O)=C5)=C2)C
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| InChi Key |
WKDACQVEJIVHMZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H32N4O3S/c1-5-36(34,35)21-8-6-7-19(14-21)23-15-22(28(33)30-20-9-11-32(4)12-10-20)18(3)26-25(23)24-13-17(2)16-29-27(24)31-26/h6-8,13-16,20H,5,9-12H2,1-4H3,(H,29,31)(H,30,33)
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| Chemical Name |
5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9816 mL | 9.9081 mL | 19.8161 mL | |
| 5 mM | 0.3963 mL | 1.9816 mL | 3.9632 mL | |
| 10 mM | 0.1982 mL | 0.9908 mL | 1.9816 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00807677 | Completed | Drug: TAK-901 | Acute Myeloid Leukemia Acute Lymphoblastic Leukemia |
Millennium Pharmaceuticals, Inc. | March 2009 | Phase 1 |
| NCT00935844 | Completed | Drug: TAK-901 | Advanced Solid Tumors Lymphoma |
Millennium Pharmaceuticals, Inc. | October 2009 | Phase 1 |
A, chemical structure of TAK-901. B, TAK-901 inhibition of Aurora A and B kinase/coactivator complexes and kinetic data of the Aurora B/INCENP enzyme complex. C, kinase inhibition profile of TAK-901. D, enzyme reaction progression curves showing TAK-901 time-dependent binding to (D) and dissociation (E) from Aurora B/INCENP enzyme complex.Mol Cancer Ther. 2013 Apr;12(4):460-70. |
TAK-901 inactivates cellular Aurora B kinase and inhibits cell proliferation. A, immunoblot analysis of histone H3 phosphorylation in PC3 cells treated with TAK-901. B, PC3 cells were incubated for 48 hours with dimethyl sulfoxide or 0.2 μmol/L TAK-901 and stained for actin (green) and DNA (blue). C, DNA content histograms of HL60 cells after incubation for 48 hours with a concentration dilution series of TAK-901. D, TAK-901 EC50values for cell proliferation (DNA synthesis) inhibition in cells.Mol Cancer Ther. 2013 Apr;12(4):460-70. |
Profile of various TAK-901 kinase targets. A, MV4-11 cells, 2 μmol/L FLT3/MTK inhibitor. B, KATO-III cells, 10 μmol/L Aurora B inhibitor. C, profile of TAK-901 cellular activity against Aurora B kinase and several cross-reacting kinases. EC50values derived from dose–response immunoblotting or cellular reporter.Mol Cancer Ther. 2013 Apr;12(4):460-70. |
In vivoantitumor activity of TAK-901 in human tumor and leukemia xenograft models.Mol Cancer Ther. 2013 Apr;12(4):460-70. |
In vivoeffects of TAK-901 on Aurora B pharmacodynamic markers. A, histone H3 phosphorylation in nude rat A2780 xenograft tumors.B, polyploidy in nude mice A2780 xenograft tumors.Mol Cancer Ther. 2013 Apr;12(4):460-70. |
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