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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Barasertib-HQPA [722544-51-6]

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Referência HY-10126-1mL

Tamanho : 10mM/1mL

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Marca : MedChemExpress

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Description

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]
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]
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]
MOLM-13	IC₅₀	1 nM Compound: AZD1152-HQPA	Inhibition of clonogenic growth in human MOLM-13 cells incubated for 10 days Inhibition of clonogenic growth in human MOLM-13 cells incubated for 10 days	[PMID: 17495131]
MOLM-13	IC₅₀	12 nM Compound: AZD1152-HQPA	Inhibition of cell proliferation of human MOLM-13 cells incubated for 48 hrs by 3H-thymidine uptake assay Inhibition of cell proliferation of human MOLM-13 cells incubated for 48 hrs by 3H-thymidine uptake assay	[PMID: 17495131]
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	2.8 nM Compound: AZD1152-HQPA	Inhibition of clonogenic growth in human MV4-11 cells incubated for 10 days Inhibition of clonogenic growth in human MV4-11 cells incubated for 10 days	[PMID: 17495131]
MV4-11	IC₅₀	8 nM Compound: AZD1152-HQPA	Inhibition of cell proliferation of human MV4-11 cells incubated for 48 hrs by 3H-thymidine uptake assay Inhibition of cell proliferation of human MV4-11 cells incubated for 48 hrs by 3H-thymidine uptake assay	[PMID: 17495131]
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]
SW-620	IC₅₀	0.017 μM Compound: 7, AZD-1152 HQPA	Inhibition of aurora B in human SW620 cells assessed as inhibition of histone H3 phosphorylation Inhibition of aurora B in human SW620 cells assessed as inhibition of histone H3 phosphorylation	[PMID: 19320489]
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.

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.

Essai clinique

Masse moléculaire

507.56

Formule

C₂₆H₃₀FN₇O₃

CAS No.

722544-51-6

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

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
10 mM	0.1970 mL	0.9851 mL	1.9702 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.

Pureté et documentation

Purity: 98.90%

Fiche technique (275 KB) SDS (396 KB)

COA (246 KB) HNMR (283 KB) RP-HPLC (263 KB) MS (68 KB) Elemental Analysis Report (103 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Yang, Jing., et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 15;110(6):2034-40. [Content Brief]

[2]. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. [Content Brief]

[3]. Zekri A, et al. AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Tumour Biol. 2015 Feb;36(2):623-32. [Content Brief]

[4]. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8. [Content Brief]

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Barasertib-HQPA [722544-51-6]

Referência HY-10126-1mL

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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