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TAK-901

Cat. No. M2154
TAK-901 Structure
Synonym:

TAK901

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 45  USD45 In stock
5mg USD 85  USD85 In stock
10mg USD 150  USD150 In stock
50mg USD 410  USD410 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.

Customer Product Validations & Biological Datas
Source Anticancer Res (2017). Figure 1. TAK-901
Method FACS analysis
Cell Lines HCT116 cells
Concentrations 100 nM
Incubation Time 72 h
Results Induction of polyploidy was also detected by FACS analysis; 2N and 4N cells were observed in DMSO-treated HCT116 cells, while mainly 4N and 8N were observed in TAK-901- or AZD1152-HQPA-treated HCT116 cells
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 504.64
Formula C28H32N4O3S
CAS Number 934541-31-8
Purity 99.89%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

[1] Farrell P, et al. Mol Cancer Ther. Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor.

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Keywords: TAK-901, TAK901 supplier, Aurora Kinase, inhibitors

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