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Technical Data
| Formula | C28H32N4O3S |
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| Molecular Weight | 504.64 | CAS No. | 934541-31-8 | |
| Solubility (25°C)* | In vitro | DMSO | 101 mg/mL (200.14 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1. | |||||||||||
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| Targets |
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| In vitro | TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901 binding to Aurora B-INCENP is determined to be 0.02 nM. TAK-901 induces inhibition of cell proliferation in cultured human cancer cell lines from different tissues with IC50s ranging from 40 to 500nM. Consistent with Aurora B inhibition, TAK-901 treatment produces polyploidy in human PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured by immunofluorescence and flow cytometry. Examination of a broad panel of kinases reveals that multiple kinases, including FLT3, FGFR and the Src family kinases, are inhibited by TAK-901 with IC50 values similar to those for Aurora A and B. In cells, TAK-901 suppresses the Flt3 and FGFR2 autophosphorylation with IC50 values close to that of Aurora B as measured by cellular histone H3 phosphorylation, whereas the IC50s for inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of pathway specific reporter-based cell models, TAK-901 inhibits the NFkB and JAK/STAT pathways with submicromolar potency. [1] |
Protocol (from reference)
References
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Selleck's TAK-901 has been cited by 10 publications
| DELs enable the development of BRET probes for target engagement studies in cells [ Cell Chem Biol, 2023, 30(8):987-998.e24] | PubMed: 37490918 |
| Inhibitors of One or More Cellular Aurora Kinases Impair the Replication of Herpes Simplex Virus 1 and Other DNA and RNA Viruses with Diverse Genomes and Life Cycles [ Microbiol Spectr, 2023, 11(1):e0194322] | PubMed: 36537798 |
| Selective Impact of ALK and MELK Inhibition on ERα Stability and Cell Proliferation in Cell Lines Representing Distinct Molecular Phenotypes of Breast Cancer [ bioRxiv, 2023, 10.1101/2023.12.19.572304] | PubMed: none |
| A chemical genetic screen identifies Aurora kinases as a therapeutic target in EGFR T790M negative, gefitinib-resistant head and neck squamous cell carcinoma (HNSCC) [ EBioMedicine, 2021, 64:103220] | PubMed: 33529999 |
| A chemical genetic screen identifies Aurora kinases as a therapeutic target in EGFR T790M negative, gefitinib-resistant head and neck squamous cell carcinoma (HNSCC) [ EBioMedicine, 2021, 64:103220] | PubMed: 33529999 |
| Differential reprogramming of breast cancer subtypes in 3D cultures and implications for sensitivity to targeted therapy [ Sci Rep, 2021, 11(1):7259] | PubMed: 33790333 |
| Tumor immunological phenotype signature-based high-throughput screening for the discovery of combination immunotherapy compounds [ Sci Adv, 2021, 7(4)eabd7851] | PubMed: 33523948 |
| A High-Content Screen Identifies TPP1 and Aurora B as Regulators of Axonal Mitochondrial Transport. [ Cell Rep, 2019, 28(12):3224-3237] | PubMed: 31533043 |
| Network pharmacology modeling identifies synergistic Aurora B and ZAK interaction in triple-negative breast cancer [ NPJ Syst Biol Appl, 2019, 5:20] | PubMed: 31312514 |
| Bioluminescent cell-based NAD(P)/NAD(P)H assays for rapid dinucleotide measurement and inhibitor screening [ Assay Drug Dev Technol, 2014, 12(9-10):514-26] | PubMed: 25506801 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.