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Chemical Structure| 722543-31-9 Chemical Structure| 722543-31-9

Structure of Barasertib
CAS No.: 722543-31-9

Chemical Structure| 722543-31-9

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Barasertib (AZD1152) is the prodrug of Barasertib-hQPA, a highly selective Aurora B inhibitor with an IC50 of 0.37 nM. Barasertib (AZD1152) induces cancer cell growth arrest and apoptosis.

Synonyms: Azd1152

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Product Details of Barasertib

CAS No. :722543-31-9
Formula : C26H31FN7O6P
M.W : 587.54
SMILES Code : O=P(OCCN(CCCOC1=CC2=NC=NC(NC3=NNC(CC(NC4=CC=CC(F)=C4)=O)=C3)=C2C=C1)CC)(O)O
Synonyms :
Azd1152
MDL No. :MFCD15146330

Safety of Barasertib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Barasertib

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC9-ER 0.06 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR3 0.05 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR1-AZD4 0.03 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR1-AZD3 0.03 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR1-AZD2 0.03 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR1-AZD1 0.04 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
BT-474 8 nM AZD1152-HQPA inhibited cell proliferation Mol Cancer. 2010 Feb 22;9:42
MDA-MB-361 70 nM AZD1152-HQPA inhibited cell proliferation Mol Cancer. 2010 Feb 22;9:42
MDA-MB-231 105 nM AZD1152-HQPA inhibited cell proliferation and induced apoptosis Mol Cancer. 2010 Feb 22;9:42
MDA-MB-435 125 nM AZD1152-HQPA inhibited cell proliferation Mol Cancer. 2010 Feb 22;9:42
MDA-MB-468 14 nM AZD1152-HQPA inhibited cell proliferation Mol Cancer. 2010 Feb 22;9:42
HER18 20 nM 48 h AZD1152-HQPA inhibited Aurora B kinase activity, leading to mitotic catastrophe, polyploidy, and apoptosis Mol Cancer. 2010 Feb 22;9:42
11-18-GR5 0.06 µM 72 h Barasertib showed strong antiproliferative effects with IC50s in the nM range Nat Commun. 2019 Apr 18;10(1):1812
11-18-GR3 0.06 µM 72 h Barasertib showed strong antiproliferative effects with IC50s in the nM range Nat Commun. 2019 Apr 18;10(1):1812
PC9-GR5 0.04 µM 72 h Barasertib showed strong antiproliferative effects with IC50 < 0.06 µM Nat Commun. 2019 Apr 18;10(1):1812
Cord blood Lin− cells 10 nM, 100 nM, 1000 nM 2 weeks AZD1152-HQPA showed a dose-dependent effect on the growth and differentiation of cord blood progenitor cells, with no colonies detected at 1000 nM. Cancer Res. 2009 May 15;69(10):4150-8
THP-1 cells 100 nM 96 h THP-1 cells showed a low apoptotic response to AZD1152-HQPA, with more than 80% of cells remaining polyploid at 100 nM and exhibiting senescence-associated β-galactosidase activity. Cancer Res. 2009 May 15;69(10):4150-8
HL-60 cells 0–1000 nM 96 h AZD1152-HQPA exerted anti-proliferative or cytotoxic effects in all cell lines studied, inhibited the phosphorylation of histone H3 (pHis H3) on ser10 in a dose dependent manner and resulted in cells with more than 4N DNA content. Cancer Res. 2009 May 15;69(10):4150-8
PAH-PASMCs 0.5 μM 48 h To evaluate the effect of Barasertib on proliferation and apoptosis of PAH-PASMCs. Results showed that Barasertib dose-dependently reduced proliferation of PAH-PASMCs (assessed by EdU incorporation and Ki67 labeling) and significantly decreased the resistance of PAH-PASMCs to apoptosis under serum starvation (assessed by Annexin V and TUNEL labeling). Cell Rep Med. 2025 Feb 18;6(2):101964
mouse lung fibroblasts 5 μM 48 h To assess the effect of Barasertib on fibroblast proliferation, results showed Barasertib significantly reduced BrdU incorporation EMBO Mol Med. 2020 Sep 7;12(9):e12131
human IPF lung fibroblasts 5 μM 48 h To assess the effect of Barasertib on fibroblast proliferation, results showed Barasertib significantly reduced BrdU incorporation EMBO Mol Med. 2020 Sep 7;12(9):e12131

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Patient-derived xenograft model Oral gavage and intraperitoneal injection 25 mg/kg Once daily, 3 days on and 4 days off Evaluate the inhibitory effect of TAZ and barasertib combination on tumor growth Cancer Discov. 2024 Jun 3;14(6):965-981.
Rats MCT-induced PAH model Intraperitoneal injection 30 mg/kg Three times a week from day 14 to 28 To evaluate the therapeutic effect of Barasertib in MCT-induced PAH rats. Results showed that Barasertib significantly reduced right ventricular hypertrophy (assessed by Fulton index) and right ventricular systolic pressure (RVSP) and mean pulmonary artery pressure (mPAP) (assessed by right heart catheterization). Additionally, Barasertib significantly attenuated vascular remodeling in distal pulmonary arteries (assessed by Elastica van Gieson staining). Cell Rep Med. 2025 Feb 18;6(2):101964
NOD/SCID mice HL-60 cell xenograft model Subcutaneous osmotic pump 25 mg/kg/day 1 week continuously AZD1152 at 25 mg/kg/day significantly reduced the growth of HL-60 cell xenografts, with no regrowth observed post-treatment. Cancer Res. 2009 May 15;69(10):4150-8
Nude mice Breast cancer xenograft model Intraperitoneal injection 62.5 mg/kg and 125 mg/kg Every 7 days for a cycle, administered on days 1 and 2, total of 3 cycles AZD1152 suppressed tumor growth, reduced Ki-67 expression, and increased Caspase 3 cleavage Mol Cancer. 2010 Feb 22;9:42
Nude mice CaLu-6 NSCLC human tumour xenograft model Subcutaneous osmotic mini-pump 150 mg/kg 2 consecutive days, once daily, followed by a 24-hour gap To investigate the anti-tumour efficacy of Barasertib in combination with the MEK inhibitor selumetinib. Results showed enhanced tumour growth inhibition and increased cell death when Barasertib was administered before selumetinib. Br J Cancer. 2012 Feb 28;106(5):858-66
Mice TGFα-induced pulmonary fibrosis model Intraperitoneal injection 40 mg/kg body weight Twice a day for 4 weeks To evaluate the preventive effect of Barasertib on pulmonary fibrosis, results showed Barasertib significantly reduced collagen deposition and lung weight EMBO Mol Med. 2020 Sep 7;12(9):e12131
Nude mice AA TNBC xenograft model Intraperitoneal injection 100 mg/kg Twice weekly for up to 28 days To evaluate the effect of Barasertib on the growth of AA TNBC xenografts, results showed that Barasertib significantly inhibited the growth of AA TNBC xenografts. Cell Death Dis. 2023 Jan 10;14(1):12

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.51mL

1.70mL

0.85mL

17.02mL

3.40mL

1.70mL

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