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> Barasertib-HQPA [722544-51-6]

Barasertib-HQPA [722544-51-6]

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Referencia HY-10126-5mg

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Marca : MedChemExpress

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Descripciòn

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells[1].

IC50 & Target[1]

Aurora B

0.37 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.1 μM
Compound: AAZD1152-HQPA
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 25036791]
A549 IC50
5.4 μM
Compound: AAZD1152-HQPA
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by transwell migration assay
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by transwell migration assay
[PMID: 25036791]
A549 IC50
8.3 μM
Compound: AAZD1152-HQPA
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by scratch wound model assay
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by scratch wound model assay
[PMID: 25036791]
HepG2 IC50
0.1 μM
Compound: AAZD1152-HQPA
Cytotoxicity against human HepG2 cells by SRB assay
Cytotoxicity against human HepG2 cells by SRB assay
[PMID: 25036791]
HL-60 IC50
12.7 nM
Compound: AZD1152
Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 25089810]
MOLM-13 IC50
9.7 nM
Compound: AZD1152
Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 25089810]
MV4-11 IC50
8.6 nM
Compound: AZD1152
Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 25089810]
THP-1 IC50
25.1 nM
Compound: AZD1152
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 25089810]
In Vitro

Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells[1].
Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is converted rapidly to the active Barasertib-HQPA in plasma[2].
Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line[3].
Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis[4].

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

Barasertib-HQPA Related Antibodies

Cell Proliferation Assay[1].

Cell Line: AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells.
Concentration: 0-100 nM. (Barasertib -HQPA)
Incubation Time: 48 h.
Result: IC50 values ranged from 3 nM to 40 nM.
In Vivo

Barasertib-HQPA (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors[1].
Barasertib-HQPA (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1].
Barasertib-HQPA (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P < 0.05) in immunodeficient mice[2].

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

507.56

Fòrmula

C26H30FN7O3
No. CAS
Appearance

Solid

Color

White to yellow

SMILES

O=C(CC1=NNC(NC2=C3C=CC(OCCCN(CCO)CC)=CC3=NC=N2)=C1)NC4=CC=CC(F)=C4
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : ≥ 22 mg/mL (43.34 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
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9702 mL 9.8511 mL 19.7021 mL
5 mM 0.3940 mL 1.9702 mL 3.9404 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.

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: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureza y Documentación
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