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Chemical Structure| 958852-01-2 Chemical Structure| 958852-01-2

Structure of GSK1059615
CAS No.: 958852-01-2

Chemical Structure| 958852-01-2

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GSK1059615 is a reversible inhibitor of PI3Kα/β/δ/γ and also inhibits mTOR, with IC50 values of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

Synonyms: GSK1059615

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Product Details of GSK1059615

CAS No. :958852-01-2
Formula : C18H11N3O2S
M.W : 333.36
SMILES Code : O=C(NC/1=O)SC1=C/C2=CC=C3N=CC=C(C4=CC=NC=C4)C3=C2
Synonyms :
GSK1059615
MDL No. :MFCD18074517

Safety of GSK1059615

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

Related Pathways of GSK1059615

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:5 nM

  • p110β

    PI3Kβ, IC50:0.6 nM

  • p110α

    PI3Kα, IC50:0.4 nM

  • p110δ

    PI3Kδ, IC50:2 nM

  • mTOR

    mTOR, IC50:12 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HT-p21 cells 1000 nM 4 days Inhibited cellular hypertrophy and senescent phenotype PMC5270685
FISS-derived cells 60, 30, 15, 7.5, 3.75, 1.88 μM 48 hours To evaluate the inhibitory effect of GSK-1059615 on FISS cell growth, results showed an IC50 of 4.6 μM. PMC6449919
SCC-9 cells 0.3-30 μM 48h-96h To test the effect of GSK1059615 on HNSCC cell survival, results showed that GSK1059615 dose-dependently inhibited cell survival PMC5584207
OCC1-4 primary cancer cells 3 μM 72h To test the effect of GSK1059615 on primary HNSCC cell survival, results showed that GSK1059615 was cytotoxic to all primary cancer cells PMC5584207
A253 and SQ20B cells 3 μM 72h To test the effect of GSK1059615 on other HNSCC cell survival, results showed that GSK1059615 significantly reduced cell survival PMC5584207

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SCC-9 xenograft model Intraperitoneal injection 30 mg/kg Once daily for 5 weeks To test the inhibitory effect of GSK1059615 on SCC-9 tumor growth in vivo, results showed that GSK1059615 significantly inhibited tumor growth PMC5584207

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00695448 Solid Tumours PHASE1 TERMINATED 2009-03-31 GSK Investigational Site, Nash... More >>ville, Tennessee, 37203, United States|GSK Investigational Site, Houston, Texas, 77030-4009, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

15.00mL

3.00mL

1.50mL

30.00mL

6.00mL

3.00mL

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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