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Chemical Structure| 938440-64-3 Chemical Structure| 938440-64-3

Structure of KU-0063794
CAS No.: 938440-64-3

Chemical Structure| 938440-64-3

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KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively) with no effect on PI3Ks.

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Product Details of KU-0063794

CAS No. :938440-64-3
Formula : C25H31N5O4
M.W : 465.54
SMILES Code : OCC1=CC(C2=NC3=NC(N4C[C@@H](C)O[C@@H](C)C4)=NC(N5CCOCC5)=C3C=C2)=CC=C1OC
MDL No. :MFCD11977741
InChI Key :RFSMUFRPPYDYRD-CALCHBBNSA-N
Pubchem ID :16736978

Safety of KU-0063794

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

Related Pathways of KU-0063794

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTORC1

    mTORC1, IC50:~10 nM

  • mTORC2

    mTORC2, IC50:~10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK-293 cells 30 nM 30 minutes Inhibition of S6K1 activity and phosphorylation PMC2708931
HEK-293 cells 1 μM 30 minutes Inhibition of Akt activity and phosphorylation PMC2708931
Keloid fibroblasts (KFs) 2.5 μmol/L 24 hours KU-0063794 significantly inhibited the proliferation, migration, and invasion of keloid fibroblasts and induced apoptosis. PMC3631609
Keloid fibroblasts (KFs) 10 μmol/L 24 hours KU-0063794 significantly inhibited the proliferation, migration, and invasion of keloid fibroblasts and induced apoptosis. PMC3631609
N-HCC25 cells 1 µM, 2.5 µM, 5 µM 24 hours To investigate the effect of KU-0063794 on the proliferation of N-HCC25 cells, results showed that KU-0063794 significantly inhibited cell proliferation in a dose-dependent manner and induced G1/G0 cell cycle arrest. PMC6888677
AGS 0.1 to 1000 μM 72 hours To evaluate the sensitivity of KU-0063794 in PIK3CA mutant and wild-type gastric cancer cells, results showed increased resistance to KU-0063794 in PIK3CA mutant cells under low glucose conditions. PMC4080979
HGC27 0.1 to 1000 μM 72 hours To evaluate the sensitivity of KU-0063794 in PIK3CA mutant and wild-type gastric cancer cells, results showed increased resistance to KU-0063794 in PIK3CA mutant cells under low glucose conditions. PMC4080979
MKN45 0.1 to 1000 μM 72 hours To evaluate the sensitivity of KU-0063794 in PIK3CA mutant and wild-type gastric cancer cells, results showed no significant change in sensitivity to KU-0063794 in wild-type cells under low glucose conditions. PMC4080979
NUGC4 0.1 to 1000 μM 72 hours To evaluate the sensitivity of KU-0063794 in PIK3CA mutant and wild-type gastric cancer cells, results showed no significant change in sensitivity to KU-0063794 in wild-type cells under low glucose conditions. PMC4080979

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse Wild-type and mLST8-deficient MEFs 250 μg/kg once a day for three consecutive days Suppression of cell growth and induction of G1 cell cycle arrest PMC2708931
Mice UCP1-deficient mice Intraperitoneal injection 200 mg/kg three times a week for four weeks KU-0063794 blocked CL-316,243-induced glucose uptake, indicating that glucose uptake is mediated via the mTOR pathway PMC5444022
Drosophila melanogaster y w male Drosophila Dietary supplementation 3 μM 1, 2, or 3 days To test the effect of KU-0063794 on the lifespan of Drosophila, results showed no significant effect at any dose. PMC11547029

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL

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
 

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