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Chemical Structure| 1394076-92-6 Chemical Structure| 1394076-92-6

Structure of GNE-317
CAS No.: 1394076-92-6

Chemical Structure| 1394076-92-6

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GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood–brain barrier and shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.

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Product Details of GNE-317

CAS No. :1394076-92-6
Formula : C19H22N6O3S
M.W : 414.48
SMILES Code : NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(C5(OC)COC5)S4)=N2)C=N1
MDL No. :MFCD28900677
InChI Key :XOZLHJMDLKDZAL-UHFFFAOYSA-N
Pubchem ID :70676303

Safety of GNE-317

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

Related Pathways of GNE-317

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • PI3K

In Vitro:

Cell Line
Concentration Treated Time Description References
A2058 cells 0.1, 1, 5 µM 10 hours Validation of Akt biosensor activity, showing reduced Akt activity after GNE-317 treatment PMC8804893
GSC727-1 5 μM 48 hours Reversed PMT process and inhibited PI3K/mTOR signaling pathway PMC11948001
GSC628 5 μM 48 hours Inhibited MSN expression and enhanced sensitivity to RT and TMZ PMC11948001
GSC924 5 μM 48 hours Inhibited MSN expression and enhanced sensitivity to RT and TMZ PMC11948001

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Melanoma brain metastasis model Oral gavage 2.5/12.5/25 mg/kg Once daily for 4 to 28 days Preventive use of GNE-317 significantly reduced the formation and growth of brain metastases, with low-dose group showing comparable effects to medium-dose group PMC8804893
Mice GL261 intracranial tumor model Oral 30 mg/kg Once daily for 3 days To evaluate the brain penetrance and molecular targeting efficacy of GNE-317 in the GL261 intracranial tumor model, showing 3-fold greater penetrance in tumor core, rim, and normal brain compared to GDC-0980, and enhanced inhibition of PI3K/mTOR signaling pathways. PMC4588756
Nude mice GSC924 xenograft model Oral 40 mg/kg Five times per week for two weeks Combined with RT and TMZ significantly inhibited tumor growth and prolonged survival PMC11948001
FVB mice HER2-positive breast cancer brain metastasis model Oral gavage 30 mg/kg Once daily for 20 days To evaluate the efficacy of GNE-317 in combination with muMAb 4D5, results showed that combination therapy extended survival more than either agent alone PMC5495871

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

References

 

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