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TAK-901

Cat. No. M2154

TAK-901 Structure
Size Price Availability Quantity
10mg USD 190 In stock
50mg USD 555 In stock
100mg USD 855 In stock
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Quality Control
Biological Activity

TAK-901 is an investigational, multitargeted Aurora B kinase inhibitor with potential antineoplastic activity. TAK-901 potently inhibited only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2. TAK-901 inhibited cell proliferation with effective concentration values from 40 to 500 nmol/L in various human cancer cell lines. TAK-901 suppressed cellular histone H3 phosphorylation and induced polyploidy. TAK-901 displayed potent activity against several leukemia models. In rodent xenografts, TAK-901 exhibited potent activity against multiple human solid tumor types, and complete regression was observed in the ovarian cancer A2780 model. In vivo studies showed that TAK-901 induced pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue. TAK-901 is currently in a phase I clinical trials in patients within a diverse range of cancers.

Protocol
Cell Experiment
Cell lines A2780, A375, A549, COLO-205, HCT116, PC-3 cells line
Preparation method Cell proliferation and viability assays.
Cells were plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation was determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA (Roche Diagnostics). IMR-90 immortalized lung fibroblasts were seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells were then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay was conducted as per the manufacturer's instructions (Promega). The concentration of TAK-901 required to inhibit half of the maximal effective concentration (EC50) was determined from the dose–response curves.
Concentrations 0~8 μM
Incubation time 72 h
Animal Experiment
Animal models Nude mice or rats Xenograft models
Formulation 12% Captisol, 25 mmol/L citrate, pH 3.0
Dosages 5 μL/mg twice daily
Administration intravenously
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 504.64
Formula C28H32N4O3S
CAS Number 934541-31-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor.
Farrell P, et al. Mol Cancer Ther. 2013 Apr;12(4):460-70. PMID: 23358665.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAK-901 supplier, Aurora Kinase, inhibitors

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