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Chemical Structure| 1382979-44-3 Chemical Structure| 1382979-44-3

Structure of GDC-0084
CAS No.: 1382979-44-3

Chemical Structure| 1382979-44-3

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GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

Synonyms: Paxalisib; RG7666

4.5 *For Research Use Only !

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Product Details of GDC-0084

CAS No. :1382979-44-3
Formula : C18H22N8O2
M.W : 382.42
SMILES Code : NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1
Synonyms :
Paxalisib; RG7666
MDL No. :MFCD30187522
InChI Key :LGWACEZVCMBSKW-UHFFFAOYSA-N
Pubchem ID :57384863

Safety of GDC-0084

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

Related Pathways of GDC-0084

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, Ki app:10 nM

  • p110β

    PI3Kβ, Ki app:46 nM

  • p110α

    PI3Kα, Ki app:2 nM

  • p110δ

    PI3Kδ, Ki app:3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
GBM cell lines (G111, G96, G112, U87, SF268, G122) 0.27-1.01 μM (EC50) 4 days Evaluate the antiproliferative effect of GDC-0084 in multiple GBM cell lines, EC50 range from 0.27 to 1.01 μM PMC4834666
Acanthamoeba castellanii 18 μM 48 hours Evaluate the inhibitory effect of GDC-0084 on Acanthamoeba castellanii, showing an EC50 of 18 μM. PMC6849155
Naegleria fowleri 3.7 μM (EC50) 48 hours Evaluate the inhibitory effect of GDC-0084 on Naegleria fowleri, showing an EC50 of 3.7 μM. PMC6849155
Balamuthia mandrillaris 3.7 μM (EC50) 72 hours Evaluate the inhibitory effect of GDC-0084 on Balamuthia mandrillaris, showing an EC50 of 3.7 μM. PMC6849155
PC3 cells 0.4 μM Evaluate the antiproliferative effect of GDC-0084 in PC3 cells, EC50 of 0.4 μM PMC4834666

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01547546 Glioblastoma, Glioma PHASE1 COMPLETED 2025-01-15 Los Angeles, California, 90095... More >>, United States|Boston, Massachusetts, 02114, United States|Boston, Massachusetts, 02115, United States|Houston, Texas, 77030, United States|Barcelona, 08035, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.07mL

2.61mL

1.31mL

26.15mL

5.23mL

2.61mL

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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