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Chemical Structure| 1086062-66-9 Chemical Structure| 1086062-66-9

Structure of Omipalisib
CAS No.: 1086062-66-9

Chemical Structure| 1086062-66-9

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GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

Synonyms: GSK2126458; GSK458

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Product Details of Omipalisib

CAS No. :1086062-66-9
Formula : C25H17F2N5O3S
M.W : 505.50
SMILES Code : O=S(C1=CC=C(F)C=C1F)(NC2=CC(C3=CC=C4N=CC=C(C5=CC=NN=C5)C4=C3)=CN=C2OC)=O
Synonyms :
GSK2126458; GSK458
MDL No. :MFCD16038929
InChI Key :CGBJSGAELGCMKE-UHFFFAOYSA-N
Pubchem ID :25167777

Safety of Omipalisib

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

Related Pathways of Omipalisib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    p110γ, Ki:0.06 nM

  • p110β

    p110β, Ki:0.13 nM

  • p110α

    p110α, Ki:0.019 nM

  • p110δ

    p110δ, Ki:0.024 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01725139 Idiopathic Pulmonary Fibrosis Phase 1 Completed - United Kingdom ... More >> GSK Investigational Site London, United Kingdom, SW3 6NP Less <<
NCT00972686 Solid Tumours PHASE1 COMPLETED 2015-03-31 GSK Investigational Site, San ... More >>Francisco, California, 94115, United States|GSK Investigational Site, New Brunswick, New Jersey, 08901, United States|GSK Investigational Site, Chapel Hill, North Carolina, 27599-7600, United States|GSK Investigational Site, Dallas, Texas, 75246, United States|GSK Investigational Site, Houston, Texas, 77030, United States|GSK Investigational Site, Salt Lake City, Utah, 84112-5550, United States|GSK Investigational Site, Seattle, Washington, 98109, United States|GSK Investigational Site, Amsterdam, 1066 CX, Netherlands|GSK Investigational Site, Utrecht, 3584 CX, Netherlands Less <<
NCT01248858 Cancer Phase 1 Terminated(The reason for term... More >>ination was lack of tolerability and efficacy of the combination treatment) Less << - United States, North Carolina ... More >> GSK Investigational Site Chapel Hill, North Carolina, United States, 27599-7305 United States, Tennessee GSK Investigational Site Nashville, Tennessee, United States, 37203 Canada, Ontario GSK Investigational Site Toronto, Ontario, Canada, M5G 2M9 Italy GSK Investigational Site Milano, Lombardia, Italy, 20132 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.78mL

3.96mL

1.98mL

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

References

 

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