ZM-447439 [331771-20-1]
Referência HY-10128-10mg
Tamanho : 10mg
Marca : MedChemExpress
ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
ZM-447439 Chemical Structure
CAS No. : 331771-20-1
This product is a controlled substance and not for sale in your territory.
Based on 4 publication(s) in Google Scholar
Voir tous les produits spécifiques à Isoform Aurora Kinase:
Description |
ZM-447439 is an aurora kinase inhibitor with IC50s of 110 and 130 nM for aurora A and B, respectively. |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
|
||||||||||||
In Vitro |
Cells treated with ZM-447439 progress through interphase, enter mitosis normally, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and inhibit mitotic phosphorylation of histone H3. ZM-447439 prevents chromosome alignment and segregation. ZM-447439 compromises spindle checkpoint function. ZM-447439 inhibits kinetochore localization of BubR1, Mad2, and Cenp-E[1]. Inhibition of Aurora kinase by ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinoma cells. Multipolar spindles are induced in these ZM-treated G2/M-arrested cells with accumulation of 4N/8N DNA, similar to cells with genetically suppressed Aurora-B. ZM-447439 treatment induces cell apoptosis. ZM-447439 inhibition of Aurora kinase is potently in association with decrease of Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Masse moléculaire |
513.59 |
||||||||||||
Formule |
C29H31N5O4 |
||||||||||||
CAS No. |
331771-20-1 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
White to gray |
||||||||||||
SMILES |
O=C(NC1=CC=C(NC2=C(C(C=C3OCCCN4CCOCC4)=NC=N2)C=C3OC)C=C1)C5=CC=CC=C5 |
||||||||||||
Livraison | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Stockage |
|
||||||||||||
Solvant et solubilité |
In Vitro:
DMSO : 25 mg/mL (48.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 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).
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.
|
||||||||||||
Pureté et documentation |
Purity: 99.19% |
||||||||||||
Références |
|
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 | 1.9471 mL | 9.7354 mL | 19.4708 mL | 48.6770 mL |
5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7354 mL | |
10 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL | 4.8677 mL | |
15 mM | 0.1298 mL | 0.6490 mL | 1.2981 mL | 3.2451 mL | |
20 mM | 0.0974 mL | 0.4868 mL | 0.9735 mL | 2.4338 mL | |
25 mM | 0.0779 mL | 0.3894 mL | 0.7788 mL | 1.9471 mL | |
30 mM | 0.0649 mL | 0.3245 mL | 0.6490 mL | 1.6226 mL | |
40 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2169 mL |
ZM-447439 Related Classifications
- Cell Cycle/DNA Damage Epigenetics Apoptosis
- Aurora Kinase Apoptosis