1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. TAS-119

TAS-119 

Cat. No.: HY-137377 Purity: 98.27%
Handling Instructions

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

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

TAS-119 Chemical Structure

TAS-119 Chemical Structure

CAS No. : 1453099-83-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 446 In-stock
Estimated Time of Arrival: December 31
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites[1].

IC50 & Target[1]

Aurora A

1 nM (IC50)

Aurora B

95 nM (IC50)

In Vitro

TAS-119 enhances the antiproliferative effect of Paclitaxel in a variety of human cancer cell lines, including Paclitaxel-resistant cells[1].
TAS-119 (30-300 nM) dose dependently enhances cell growth inhibition by three taxanes (Paclitaxel, Docetaxel, and Cabazitaxel) in HeLa cells. TAS-119 induces mitotic accumulation predominantly in tumor cells, compared with that in normal diploid fibroblasts[1].

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

In Vivo

TAS-119 (5-30 mg/kg; oral administration; twice daily on day 1 and everyday on day 2) treatment induces phosphorylated histone H3 (pHH3) in nude rats with the HeLa-luc xenografts[1].

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

Animal Model: Nude rats injected with HeLa-luc cells[1]
Dosage: 5 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: Oral administration; twice daily on day 1 and everyday on day 2
Result: Induced pHH3 at all doses in nude rats with the HeLa-luc xenografts.
Molecular Weight

506.36

Formula

C₂₃H₂₂Cl₂FN₅O₃

CAS No.

1453099-83-6

SMILES

O=C(C1(CC2=NC(NC3=NNC(C)=C3)=C(F)C=C2)CCN(C(C4=CC=CC(Cl)=C4Cl)=O)CC1)O

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 : 50 mg/mL (98.74 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9749 mL 9.8744 mL 19.7488 mL
5 mM 0.3950 mL 1.9749 mL 3.9498 mL
10 mM 0.1975 mL 0.9874 mL 1.9749 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.11 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TAS-119TAS119TAS 119Aurora KinaseAurora-AtaxanesPaclitaxelphosphorylatedhistone-H3antitumorInhibitorinhibitorinhibit

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Product Name:
TAS-119
Cat. No.:
HY-137377
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