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Barasertib (AZD1152-HQPA) - ≥97%, high purity , CAS No.722544-51-6, Inhibitor of aurora kinase B

Moligand™
≥97%

CAS#: 722544-51-6
Formula: C₂₆H₃₀FN₇O₃
Molecular Weight: 507.56
MDL number: MFCD10687152
PubChem CID: 16007391

Item Number

A127799

Grouped product items
SKU	Size	Availability	Price
A127799-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$75.90
A127799-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$314.90
A127799-250mg	250mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,417.90

Potent, selective Aurora B kinase inhibitor

View related series

aurora kinase B Inhibitor

Basic Description

Synonyms	722544-51-6\|AZD1152-HQPA\|barasertib-hQPA\|AZD-1152HQPA\|Barasertib (AZD1152-HQPA)\|defosbarasertib\|2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide\|UNII-29P8LWS24N\|AZD-1152-HQPA\|INH 34\|INH-34
Specifications & Purity	≥97%
Storage Temp	Store at -20°C
Shipped In	Dry ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of aurora kinase B
Product Description	AZD1152-HQPA is the active metabolite of AZD-1152, AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A. A highly selective ARK-2 inhibitor

Associated Targets

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

IUPAC Name	2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide
INCHI	InChI=1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33)
InChi Key	QYZOGCMHVIGURT-UHFFFAOYSA-N
Canonical SMILES	CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
Isomeric SMILES	CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
WGK Germany	3
PubChem CID	16007391
Molecular Weight	507.56

CAS Registry No.

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PubChem CID

ChEMBL Ligand

RCSB PDB Ligand

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Certificate of Analysis(COA)

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Lot Number	Certificate Type	Date	Item
G1629025	Certificate of Analysis	Dec 11, 2023	A127799

Solubility

DMSO ≥100mg/mL Water ≥100mg/mL Ethanol ≥2.8mg/mL

Refractive Index

1.68

Boil Point(°C)

796.7° C at 760 mmHg

References

1. Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ et al.. (2007) Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.. J Med Chem, 50 (9): (2213-24). [PMID:17373783]
2. Schwartz GK, Carvajal RD, Midgley R, Rodig SJ, Stockman PK, Ataman O, Wilson D, Das S, Shapiro GI. (2013) Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors.. Invest New Drugs, 31 (2): (370-80). [PMID:22661287]
3. Floc'h N, Ashton S, Taylor P, Trueman D, Harris E, Odedra R, Maratea K, Derbyshire N, Caddy J, Jacobs VN et al.. (2017) Optimizing Therapeutic Effect of Aurora B Inhibition in Acute Myeloid Leukemia with AZD2811 Nanoparticles.. Mol Cancer Ther, 16 (6): (1031-1040). [PMID:28292940]
4. Mitchell E et al.. (2020) XMU-MP-1 induces growth arrest in a model human mini-organ and antagonises cell cycle-dependent paclitaxel cytotoxicity.. Cell Div, 15 (11). [PMID:32973917]

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