Structure of Barasertib
CAS No.: 722543-31-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
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 |
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 |
Tags: Barasertib | AZD1152 | AZD 1152 | AZD-1152 | Aurora Kinase | Apoptosis | colon | breast | lung | cancer | leukemia | inhibitor | 722543-31-9 |
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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