1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. TAK-901

TAK-901 

Cat. No.: HY-12201 Purity: 99.80%
Handling Instructions

TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.

For research use only. We do not sell to patients.

TAK-901 Chemical Structure

TAK-901 Chemical Structure

CAS No. : 934541-31-8

Size Price Stock Quantity
5 mg USD 126 In-stock
Estimated Time of Arrival: December 31
10 mg USD 222 In-stock
Estimated Time of Arrival: December 31
50 mg USD 696 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 2 publication(s) in Google Scholar

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Description

TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.

IC50 & Target[1]

Aurora A

21 nM (IC50)

Aurora B

15 nM (IC50)

In Vitro

TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistent with Aurora B inhibition, TAK-901 suppresses cellular histone H3 phosphorylation and induces polyploidy. In various human cancer cell lines, TAK-901inhibits cell proliferation with effective concentration values from 40 to 500 nM. Examination of a broad panel of kinases in biochemical assays reveals inhibition of multiple kinases. However, TAK-901 potently inhibits only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2[1].

In Vivo

In rodent xenografts, TAK-901 exhibits potent activity against multiple human solid tumor types, and complete regression is observed in the ovarian cancer A2780 model. TAK-901 also displayed potent activity against several leukemia models. TAK-901 induces pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue[1].

Clinical Trial
Molecular Weight

504.64

Formula

C₂₈H₃₂N₄O₃S

CAS No.

934541-31-8

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.96 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9816 mL 9.9081 mL 19.8161 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Enzyme activities of Aurora A/TPX2 and Aurora B/INCENP complexes are assayed at room temperature in buffer containing serially diluted TAK-901, and the product is quantified using IMAP detection reagents. Aurora A/TPX2 (2 nM) is assayed with 100 nM FL-Kemptide and 1 mM ATP. Aurora B/INCENP (0.8 nM) is assayed with 100 nM 5-carboxy-fluorescein-GRTGRRNSI-NH2 (FL-PKAtide) and 10 mM ATP. For time-dependent inhibition, Aurora B/INCENP is incubated with TAK-901 for 1 hour at room temperature followed by addition of 150 mM ATP to initiate the reaction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cells are plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation is determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA. IMR-90 immortalized lung fibroblasts are seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells are then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay is conducted[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Tumor-bearing mice or rats are treated intravenously twice daily (b.i.d.) with either vehicle or TAK-901 on 2 consecutive days per week or every other day for 2 or 3 cycles. The antitumor activity of TAK-901 in human tumor and leukemia xenograft models are monitored[1].

Nude rats bearing A2780 tumors averaging 250 to 500 mg receive an intravenous dose of TAK-901. Plasma samples are collected by terminal cardiac puncture under CO2 anesthesia. Tumors are dissected and snap-frozen at -80°C[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.80%

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TAK-901
Cat. No.:
HY-12201
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