AZD-1152HQPA - CAS 722544-51-6
Catalog number: 722544-51-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C26H30FN7O3
Molecular Weight:
507.56
COA:
Inquire
Targets:
Aurora Kinase
Description:
AZD-1152HQPA is an active metabolite of Barasertib (AZD-1152), which is a novel acetanilide-substituted pyrazole-aminoquinazoline prodrug that is converted rapidly to the active drug AZD-1152 hydroxy-QPA (AZD1152-HQPA) in human plasma. AZD1152-HQPA is a specific inhibitor of the enzymatic activity of Aurora kinase, with selectivity for Aurora B. AZD-1152 was active against a variety of solid tumors including colon, breast, and lung cancers.
Publication citing BOC Sciences Products
1. Adsorption and reduction of roxarsone on magnetic greigite (Fe3S4): Indispensable role of structural sulfide
2. Nutrient uptake, biomass yield and quantitative analysis of aliphatic aldehydes in cilantro plants
3. Developing member, method of producing the same, process cartridge and electrophotographic image forming apparatus
4. Design and development of permeation enhancer containing self-nanoemulsifying drug delivery system (SNEDDS) for ceftriaxone sodium improved oral pharmacokinetics
5. Contaminants of emerging concern in a freeze-thaw river during the spring flood
6. Removal of acutely hazardous pharmaceuticals from water using multi-template imprinted polymer adsorbent

>> More

Purity:
0.98
Appearance:
Light yellow to yellow solid
Synonyms:
AZD-2811; AZD 2811; AZD2811; AZD-1152HQPA; AZD 1152HQPA; AZD1152HQPA; AZD1152 HQPA; AZD1152-HQPA; AZD1152HQPA.
MSDS:
Inquire
InChIKey:
QYZOGCMHVIGURT-UHFFFAOYSA-N
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)
Canonical SMILES:
CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
Current Developer:
AstraZeneca, Inc.
1.[Inhibitors of aurora kinases].
Pinel S;Barbault-Foucher S;Lott-Desroches MC;Astier A Ann Pharm Fr. 2009 Mar;67(2):69-77. doi: 10.1016/j.pharma.2008.12.005. Epub 2009 Feb 23.
Aurora kinases (A, B and C) are proteins expressed only in cells which divide actively and their increase is a factor of bad prognosis in cancer. They regulate the maturation of centrosomes, the separation and the condensation of chromosomes, mitotic checkpoint and cytokinesis. The inhibition of aurora kinases, by powerful and selective inhibitors, is due to the formation of abnormal cells which are eliminated by apoptosis. The purpose of this article is to present the role, the antitumor activity and the tolerability of these inhibitors. They can be administered orally or intravenously, on weekly or monthly schedules. In our knowledge, twelve molecules are evaluated at the present time and will be discussed only the most advanced namely: VX-680, ZM 447439, MLN 8054, AZD 1152, PHA 739358, SU 6668 and AT 9283. The main indications are breast, colon, lung, pancreas and bladder cancers as well as hematologic tumors such as leukemia (ALL, AML, CML) and lymphoma. These inhibitors can be associated with other chemotherapies. They seem well tolerated; the reported side effects are digestive disorders (diarrhea), fever, asthenia, alopecia, slumber, neutropenia, myelosuppression and disturbance of the biological markers.
2.Aurora kinase inhibitor nanoparticles target tumors with favorable therapeutic index in vivo.
Ashton S;Song YH;Nolan J;Cadogan E;Murray J;Odedra R;Foster J;Hall PA;Low S;Taylor P;Ellston R;Polanska UM;Wilson J;Howes C;Smith A;Goodwin RJ;Swales JG;Strittmatter N;Takáts Z;Nilsson A;Andren P;Trueman D;Walker M;Reimer CL;Troiano G;Parsons D;De Witt D;Ashford M;Hrkach J;Zale S;Jewsbury PJ;Barry ST Sci Transl Med. 2016 Feb 10;8(325):325ra17. doi: 10.1126/scitranslmed.aad2355.
Efforts to apply nanotechnology in cancer have focused almost exclusively on the delivery of cytotoxic drugs to improve therapeutic index. There has been little consideration of molecularly targeted agents, in particular kinase inhibitors, which can also present considerable therapeutic index limitations. We describe the development of Accurin polymeric nanoparticles that encapsulate the clinical candidate AZD2811, an Aurora B kinase inhibitor, using an ion pairing approach. Accurins increase biodistribution to tumor sites and provide extended release of encapsulated drug payloads. AZD2811 nanoparticles containing pharmaceutically acceptable organic acids as ion pairing agents displayed continuous drug release for more than 1 week in vitro and a corresponding extended pharmacodynamic reduction of tumor phosphorylated histone H3 levels in vivo for up to 96 hours after a single administration. A specific AZD2811 nanoparticle formulation profile showed accumulation and retention in tumors with minimal impact on bone marrow pathology, and resulted in lower toxicity and increased efficacy in multiple tumor models at half the dose intensity of AZD1152, a water-soluble prodrug of AZD2811. These studies demonstrate that AZD2811 can be formulated in nanoparticles using ion pairing agents to give improved efficacy and tolerability in preclinical models with less frequent dosing.
3.Optimizing Therapeutic Effect of Aurora B Inhibition in Acute Myeloid Leukemia with AZD2811 Nanoparticles.
Floc'h N;Ashton S;Taylor P;Trueman D;Harris E;Odedra R;Maratea K;Derbyshire N;Caddy J;Jacobs VN;Hattersley M;Wen S;Curtis NJ;Pilling JE;Pease EJ;Barry ST Mol Cancer Ther. 2017 Jun;16(6):1031-1040. doi: 10.1158/1535-7163.MCT-16-0580. Epub 2017 Mar 14.
Barasertib (AZD1152), a highly potent and selective aurora kinase B inhibitor, gave promising clinical activity in elderly acute myeloid leukemia (AML) patients. However, clinical utility was limited by the requirement for a 7-day infusion. Here we assessed the potential of a nanoparticle formulation of the selective Aurora kinase B inhibitor AZD2811 (formerly known as AZD1152-hQPA) in preclinical models of AML. When administered to HL-60 tumor xenografts at a single dose between 25 and 98.7 mg/kg, AZD2811 nanoparticle treatment delivered profound inhibition of tumor growth, exceeding the activity of AZD1152. The improved antitumor activity was associated with increased phospho-histone H3 inhibition, polyploidy, and tumor cell apoptosis. Moreover, AZD2811 nanoparticles increased antitumor activity when combined with cytosine arabinoside. By modifying dose of AZD2811 nanoparticle, therapeutic benefit in a range of preclinical models was further optimized. At high-dose, antitumor activity was seen in a range of models including the MOLM-13 disseminated model. At these higher doses, a transient reduction in bone marrow cellularity was observed demonstrating the potential for the formulation to target residual disease in the bone marrow, a key consideration when treating AML.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aurora Kinase Products

CAS 945595-80-2 AMG-900

AMG-900
(CAS: 945595-80-2)

AMG 900 is a small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to ...

CAS 422513-13-1 Hesperadin

Hesperadin
(CAS: 422513-13-1)

Hesperadin is  an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was...

CAS 934353-76-1 ENMD-2076

ENMD-2076
(CAS: 934353-76-1)

ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has be...

CAS 827318-97-8 Danusertib

Danusertib
(CAS: 827318-97-8)

Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the A...

CAS 934541-31-8 TAK-901

TAK-901
(CAS: 934541-31-8)

TAK-901 is a small-molecule inhibitor of the serine-threonine kinase Aurora B with potential antineoplastic activity. Aurora B kinase inhibitor TAK-901 binds to...

CAS 1028486-01-2 Alisertib

Alisertib
(CAS: 1028486-01-2)

MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with pote...

CAS 1094069-99-4 SCH-1473759

SCH-1473759
(CAS: 1094069-99-4)

SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and gen...

CAS 1207293-36-4 BI-847325

BI-847325
(CAS: 1207293-36-4)

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B...

Chemical Structure

CAS 722544-51-6 AZD-1152HQPA

Quick Inquiry

Verification code

Featured Items