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Barasertib

Catalog No. T14371   CAS 722543-31-9
Synonyms: AZD1152

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

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Barasertib Chemical Structure
Barasertib, CAS 722543-31-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 42.00
5 mg In stock $ 68.00
10 mg In stock $ 118.00
25 mg In stock $ 219.00
50 mg In stock $ 386.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
Targets&IC50 Aurora B:0.37 nM
In vitro 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 appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM and it also 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 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 causes significant accumulation of cells with 4N/8N DNA content in KMS12 and U266 and induces apoptosis in KMS18 and U266. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[1]. AZD1152 in combination with DEX, has negative effects on cell viability in comparison with single agent in PMI8226, KMS11 and U266[3].
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]. AZD1152 (25 mg/kg/day) treatment reduces xenograft levels such that they are slightly lower levels than after the first round of treatment, but this is not statistically significant indicating that residual cells might be more resistant to a second cycle of AZD1152[4]. 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].
Synonyms AZD1152
Molecular Weight 587.54
Formula C26H31FN7O6P
CAS No. 722543-31-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33 mg/mL (56.17 mM)

TargetMolReferences and Literature

1. Yang J, et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 2. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. 3. Evans RP, et al. The selective Aurora B kinase inhibitor AZD1152 is a potential new treatment for multiple myeloma. Br J Haematol. 2008 Feb;140(3):295-302. 4. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Epigenetics Compound Library Inhibitor Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Drug Repurposing Compound Library Clinical Compound Library

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Keywords

Barasertib 722543-31-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase breast cancer colon Inhibitor AZD 1152 leukemia lung inhibit AZD-1152 AZD1152 inhibitor

 

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