Tozasertib [639089-54-6]
Cat# HY-10161-50mg
Size : 50mg
Brand : MedChemExpress
Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
For research use only. We do not sell to patients.
Tozasertib Chemical Structure
CAS No. : 639089-54-6
This product is a controlled substance and not for sale in your territory.
Based on 12 publication(s) in Google Scholar
View All Aurora Kinase Isoform Specific Products:
Description |
Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively. |
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IC50 & Target[1] |
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In Vitro |
Tozasertib induces similar cytotoxicity with IC50 of approximately 300 nM and exhibits an AUR B-like inhibitory phenotype of G2/M arrest, endoreduplication and apoptosis in BaF3 cells transfected with ABL or FLT-3 (mutant and wild type) kinases. Tozasertib prevents the CAL-62 proliferation in a time-dependent manner. Tozasertib treatment for 14 days significantly decreases the number and size of colonies by approximately 70% in the 8305C and 90% in the CAL-62, 8505C and BHT-101. Treatment of the different ATC cells with Tozasertib inhibits proliferation with the IC50 between 25 and 150 nM. The Tozasertib significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that Tozasertib induces apoptosis in the different cell lines. CAL-62 cells exposed for 12 hours to Tozasertib show an accumulation of cells with ≥ 4N DNA content. Time-lapse analysis demonstrates that Tozasertib-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following Tozasertib treatment[2]. Tozasertib has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
464.59 |
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Formula |
C23H28N8OS |
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CAS No. |
639089-54-6 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
CC1=CC(NC2=NC(SC3=CC=C(C=C3)NC(C4CC4)=O)=NC(N5CCN(CC5)C)=C2)=NN1 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
4°C, protect from light *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light) |
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Solvent & Solubility |
In Vitro:
DMSO : ≥ 106.67 mg/mL (229.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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).
*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
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.
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Purity & Documentation |
Purity: 99.94% |
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References |
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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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1524 mL | 10.7622 mL | 21.5244 mL | 53.8109 mL |
5 mM | 0.4305 mL | 2.1524 mL | 4.3049 mL | 10.7622 mL | |
10 mM | 0.2152 mL | 1.0762 mL | 2.1524 mL | 5.3811 mL | |
15 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5874 mL | |
20 mM | 0.1076 mL | 0.5381 mL | 1.0762 mL | 2.6905 mL | |
25 mM | 0.0861 mL | 0.4305 mL | 0.8610 mL | 2.1524 mL | |
30 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
40 mM | 0.0538 mL | 0.2691 mL | 0.5381 mL | 1.3453 mL | |
50 mM | 0.0430 mL | 0.2152 mL | 0.4305 mL | 1.0762 mL | |
60 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8968 mL | |
80 mM | 0.0269 mL | 0.1345 mL | 0.2691 mL | 0.6726 mL | |
100 mM | 0.0215 mL | 0.1076 mL | 0.2152 mL | 0.5381 mL |
Tozasertib Related Classifications
- Cell Cycle/DNA Damage Epigenetics Autophagy
- Aurora Kinase Autophagy