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Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA)

Item no.	S1147-10000
Manufacturer	Selleckchem
CASRN	722544-51-6
Amount	10 g
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Heart & Blood Cancer Bone Cancer
Type	Inhibitors
Smiles	CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	AZD2811,INH-34,Barasertib-HQPA ,Defosbarasertib
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	507, 56
Administration	Intraperitoneal injection 4 times a week or every another day
Animal Models	Female immune-deficient BALB/c nude mice subcutaneously injected with MOLM13 cells
Cell lines	HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1, and K562 cells
Clinical Trials	A Phase I study to assess the safety and tolerability of AZD1152-HQPA in combination with low dose cytosine arabinoside (LDAC) in patients with acute myeloid leukaemia (AML) has been completed.
Concentrations	Dissolved in DMSO, final concentrations ca.100 nM
Dosages	5 or 25 mg/kg
Formulation	Dissolved in 3M Tris, pH 9.0, at a concentration of 2.5 mg/mL
IC50	0.37 nM [1], 0.37 nM [1], 0.37 nM [1], 0.37 nM [1], 0.37 nM [1], 0.37 nM [1]
In vitro	AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 uM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying ca.100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 uM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner. [1]
In vivo	Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells. [1] In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner. [2]
Incubation Time	24 or 48 hours
Method	Cells are exposed to various concentrations of AZD1152 for 24 or 48 hours. Cell proliferation is measured by 3H-thymidine uptake (isotope added 6 hours before harvest), and the concentration that induced 50% growth inhibition (IC50) is calculated from dose-response curves. Cell cycle analysis is performed by flow cytometry. Cell apoptosis is measured by annexin Vâ€“FITC apoptosis detection kit.
Solubility (25C)	DMSO 102 mg/mL, Water <1 mg/mL, Ethanol 3 mg/mL
Information	Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Chemical Name	2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide

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S1147-10000-datasheet.pdf

S1147-10000-safety-datasheet.pdf