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Chemical Structure| 1224887-10-8 Chemical Structure| 1224887-10-8

Structure of GSK2256098
CAS No.: 1224887-10-8

Chemical Structure| 1224887-10-8

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GSK2256098, is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

Synonyms: GTPL7939

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Product Details of GSK2256098

CAS No. :1224887-10-8
Formula : C20H23ClN6O2
M.W : 414.89
SMILES Code : O=C(NOC)C1=CC=CC=C1NC2=CC(NC3=CC(C)=NN3C(C)C)=NC=C2Cl
Synonyms :
GTPL7939
MDL No. :MFCD30502650
InChI Key :BVAHPPKGOOJSPU-UHFFFAOYSA-N
Pubchem ID :46214930

Safety of GSK2256098

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

Related Pathways of GSK2256098

RTK
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • FAK

    FAK, Ki:0.4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
PANC-1 0.1–10 µM 1 hour GSK2256098 inhibits FAK Y397 phosphorylation, PANC-1 cells showed lower response to GSK2256098. PMC4615113
L3.6P1 0.1–10 µM 1 hour GSK2256098 inhibits FAK Y397 phosphorylation, L3.6P1 cells showed higher response to GSK2256098. PMC4615113
GC cells 0–10 μM 2 hours Detect FAK expression levels and select the concentration with the most significant reduction in FAK protein expression for subsequent experiments PMC9379401
Ishikawa cells 0.01-10 μM 24 hours To test the sensitivity of Ishikawa and Hec1A cells to GSK2256098, Ishikawa cells were more sensitive to GSK2256098 than Hec1A cells. PMC4458384
Hec1A cells 0.01-10 μM 24 hours To test the sensitivity of Ishikawa and Hec1A cells to GSK2256098, Ishikawa cells were more sensitive to GSK2256098 than Hec1A cells. PMC4458384

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice uterine cancer model Oral 75 mg/kg daily for 4-6 weeks In the Ishikawa model, tumor growth was inhibited to a greater extent in the GSK2256098 monotherapy group compared to the Hec1A model. GSK2256098 combined with paclitaxel further reduced tumor growth and the number of tumor nodules. PMC4458384

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01138033 Cancer PHASE1 COMPLETED 2015-12-21 GSK Investigational Site, Heid... More >>elberg, Victoria, 3084, Australia|GSK Investigational Site, Nedlands, Western Australia, 6009, Australia|GSK Investigational Site, Caen Cedex 9, 14033, France|GSK Investigational Site, Villejuif, 94805, France|GSK Investigational Site, Glasgow, G61 1BD, United Kingdom|GSK Investigational Site, London, NW1 2BU, United Kingdom|GSK Investigational Site, London, W12 0HS, United Kingdom|GSK Investigational Site, London, W1G 6AD, United Kingdom|GSK Investigational Site, Manchester, M20 4BX, United Kingdom|GSK Investigational Site, Newcastle upon Tyne, NE7 7DN, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.05mL

2.41mL

1.21mL

24.10mL

4.82mL

2.41mL

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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