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Barasertib (AZD1152-HQPA) - 10mM in DMSO, high purity , CAS No.722544-51-6(DMSO), Inhibitor of aurora kinase B

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 722544-51-6(DMSO)
Molecular Weight: 507.56

In stock

Item Number

B408022

Grouped product items
SKU	Size	Availability	Price	Qty
B408022-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$238.90

Aurora B Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	AZD2811, INH-34 \| 2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide
Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	Barasertib (AZD1152-HQPA, AZD2811, INH-34) 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.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of aurora kinase B
Product Description	Information Barasertib (AZD1152-HQPA, AZD2811, INH-34) is a highly selectiveAurora Binhibitor withIC50of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1. In vitro AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. 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 ~100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. 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. 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. 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. Cell Data cell lines： Concentrations：Dissolved in DMSO, final concentrations ~100 nM Incubation Time：24 or 48 hours Powder Purity:≥95%

Product Properties

ALogP	3.493
hba_count	5
HBD Count	4
Rotatable Bond	13

Associated Targets(Human)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (3 Activities)

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (1 Activities)

Discover Target: MAP4K5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B (11 Activities)

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKC Tchem Aurora kinase C (3 Activities)

Discover Target: AURKC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (7 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (1 Activities)

Discover Target: MAP2K5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CCN(CCO)CCCOC1=CC=C2C(=NC=NC2=C1)NC3=CC(=N[NH]3)CC(=O)NC4=CC=CC(=C4)F
Molecular Weight	507.56
Reaxy-Rn	26001170
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26001170&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro Water: 78 mg/mL (181.65 mM); DMSO: 39 mg/mL (90.82 mM); Ethanol: 4 mg/mL (9.31 mM);
DMSO(mg / mL) Max Solubility	102
DMSO(mM) Max Solubility	200.96
Water(mg / mL) Max Solubility	<1

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