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Chemical Structure| 942918-07-2 Chemical Structure| 942918-07-2

Structure of GSK-1070916
CAS No.: 942918-07-2

Chemical Structure| 942918-07-2

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GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM and displays > 100-fold selectivity against the closely related Aurora A-TPX2 complex (IC50=490 nM).

Synonyms: GSK-1070916A

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Product Details of GSK-1070916

CAS No. :942918-07-2
Formula : C30H33N7O
M.W : 507.63
SMILES Code : O=C(NC1=CC=C(C2=NN(CC)C=C2C3=C4C(NC(C5=CC=CC(CN(C)C)=C5)=C4)=NC=C3)C=C1)N(C)C
Synonyms :
GSK-1070916A
MDL No. :MFCD22420815

Safety of GSK-1070916

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

Related Pathways of GSK-1070916

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • Aurora B

    Aurora B-INCENP, IC50:3.5 nM

  • Aurora C

    Aurora C-INCENP, IC50:6.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
D283 cells 0.2 µM Evaluate the effect of GSK-1070916 on the viability of D283 cells. Results showed that GSK-1070916 at 0.2 µM concentration effectively reduced cell viability. PMC11584764
HD-MB03 cells 0.033 µM Evaluate the effect of GSK-1070916 on the viability of HD-MB03 cells. Results showed that GSK-1070916 at 0.033 µM concentration effectively reduced cell viability. PMC11584764
ONS-76 cells 3 µM 24 h Evaluate the effect of GSK-1070916 on the invasion of ONS-76 cells. Results showed that GSK-1070916 at 3 µM concentration was ineffective in reducing collagen I invasion. PMC11584764
CLC4 cells 100 nM 72 h To study the effect of GSK-1070916 on the cell cycle, results showed the appearance of 8N and 16N peaks, indicating the accumulation of genome instability. PMC11601891
MHCC97L cells 100 nM 48 h To study the effect of GSK-1070916 on the cell cycle, results showed the appearance of 8N and 16N peaks, indicating the accumulation of genome instability. PMC11601891

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish larvae Zebrafish larval developmental toxicity model Water bath exposure 2, 4, 6, 8, 10 µM Daily renewal of treatment until 5 dpf Evaluate the developmental toxicity of Barasertib in zebrafish larvae. Results showed that Barasertib at tested concentrations did not cause significant developmental toxicity. PMC11584764
C57BL/6N mice Trp53KO c-MycOE HCC model Intraperitoneal injection 10 mg/kg Every 3 days for 20 days To study the effect of AZD1152 (an aurora kinase B inhibitor similar to GSK-1070916) on HCC tumors, results showed significant reduction in tumor size without causing weight loss or adverse effects. PMC11601891

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01118611 Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << Phase 1 Completed - United Kingdom ... More >> Leeds Cancer Centre at St. James's University Hospital Leeds, England, United Kingdom, LS9 7TF Barts and the London School of Medicine London, England, United Kingdom, EC1M 6BQ 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

0.98mL

19.70mL

3.94mL

1.97mL

References

 

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