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Chemical Structure| 722544-51-6 Chemical Structure| 722544-51-6

Structure of Barasertib-HQPA
CAS No.: 722544-51-6

Chemical Structure| 722544-51-6

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Barasertib-HQPA (AZD2811) is a highly selective Aurora kinase B inhibitor with an IC50 value of 0.37 nM in non-cellular assays, capable of causing cancer cell growth arrest and apoptosis.

Synonyms: AZD1152-HQPA; AZD2811; Defosbarasertib

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Product Details of Barasertib-HQPA

CAS No. :722544-51-6
Formula : C26H30FN7O3
M.W : 507.56
SMILES Code : O=C(NC1=CC=CC(F)=C1)CC2=NNC(NC3=C4C=CC(OCCCN(CC)CCO)=CC4=NC=N3)=C2
Synonyms :
AZD1152-HQPA; AZD2811; Defosbarasertib
MDL No. :MFCD17392583
InChI Key :QYZOGCMHVIGURT-UHFFFAOYSA-N
Pubchem ID :16007391

Safety of Barasertib-HQPA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Barasertib-HQPA

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • Aurora B

    Aurora B, IC50:0.37 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HD-MB03 500 nM 5 days To evaluate the inhibitory effect of Barasertib on the growth and dissemination of HD-MB03 cells in the tissue context, Barasertib significantly reduced tumor volume and proliferation volume PMC11584764
ONS-76 3 µM 24 h To screen kinase inhibitors for inhibiting MB invasion, Barasertib did not significantly reduce collagen I invasion PMC11584764
HBL 3 nM to 3 μM 3 days To evaluate the growth inhibitory effect of Barasertib-HQPA on BRAF wild-type cells, results showed significant inhibition of cell proliferation within 3 days. PMC4314759
LND1 3 nM to 3 μM 3 days To evaluate the growth inhibitory effect of Barasertib-HQPA on BRAF wild-type cells, results showed significant inhibition of cell proliferation within 3 days. PMC4314759
MBA72 3 nM to 3 μM 3 days To evaluate the growth inhibitory effect of Barasertib-HQPA on BRAF-mutated cells, results showed significant inhibition of cell proliferation within 3 days. PMC4314759
Hmel-1 3 nM to 3 μM 3 days To evaluate the growth inhibitory effect of Barasertib-HQPA on BRAF-mutated cells, results showed significant inhibition of cell proliferation within 3 days. PMC4314759
U937 cells 29 nM 72 h Barasertib-HQPA also exhibited cytotoxicity in U937 cells, inducing polyploidy and apoptosis. PMC7657165
HL-60/ara-C20 cells 70 nM 72 h Barasertib-HQPA equally inhibited the growth of HL-60/ara-C20 cells, indicating its efficacy against ara-C-resistant cells. PMC7657165
HL-60 cells 51 nM 72 h Barasertib-HQPA induced polyploidy with a subsequent induction of sub-G1 phase apoptosis, indicating the M-phase specific cytotoxicity. PMC7657165

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Zebrafish larval model Water administration 2, 4, 6, 8, 10 µM Daily administration until 5 dpf To evaluate the developmental toxicity of Barasertib in zebrafish larvae, Barasertib did not cause significant developmental toxicity PMC11584764

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03366675 Small Cell Lung Cancer PHASE2 TERMINATED 2018-10-29 Samsung Medical center, Seoul,... More >> Korea, Republic of Less <<
NCT02579226 Advanced Solid Tumours PHASE1 COMPLETED 2020-04-03 Research Site, Denver, Colorad... More >>o, 80218, United States|Research Site, Sarasota, Florida, 34232, United States|Research Site, Boston, Massachusetts, 02215, United States|Research Site, Nashville, Tennessee, 37203, United States|Research Site, Houston, Texas, 77030, United States|Research Site, Milwaukee, Wisconsin, 53226, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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