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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
Specific against	other
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
Similar products	Barasertib
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

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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S1147-10000-datasheet.pdf

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