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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 334 In-stock
Solution
10 mM * 1 mL in DMSO USD 334 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1500 In-stock
100 mg USD 2400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

TAS-119 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

TAS-119 Related Antibodies
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].

MedChemExpress (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.
Clinical Trial
Molecular Weight

506.36

Formula

C23H22Cl2FN5O3
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (98.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9749 mL 9.8744 mL 19.7488 mL 49.3720 mL
5 mM 0.3950 mL 1.9749 mL 3.9498 mL 9.8744 mL
10 mM 0.1975 mL 0.9874 mL 1.9749 mL 4.9372 mL
15 mM 0.1317 mL 0.6583 mL 1.3166 mL 3.2915 mL
20 mM 0.0987 mL 0.4937 mL 0.9874 mL 2.4686 mL
25 mM 0.0790 mL 0.3950 mL 0.7900 mL 1.9749 mL
30 mM 0.0658 mL 0.3291 mL 0.6583 mL 1.6457 mL
40 mM 0.0494 mL 0.2469 mL 0.4937 mL 1.2343 mL
50 mM 0.0395 mL 0.1975 mL 0.3950 mL 0.9874 mL
60 mM 0.0329 mL 0.1646 mL 0.3291 mL 0.8229 mL
80 mM 0.0247 mL 0.1234 mL 0.2469 mL 0.6171 mL
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TAS-119 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAS-1191453099-83-6TAS119TAS 119Aurora KinaseAurora-AtaxanesPaclitaxelphosphorylatedhistone-H3antitumorInhibitorinhibitorinhibit

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