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Chemical Structure| 1047634-65-0 Chemical Structure| 1047634-65-0

Structure of Uprosertib
CAS No.: 1047634-65-0

Chemical Structure| 1047634-65-0

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Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM, 328 nM, and 38 nM for Akt1, Akt2, and Akt3, respectively.

Synonyms: GSK2141795; GSK795

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Product Details of Uprosertib

CAS No. :1047634-65-0
Formula : C18H16Cl2F2N4O2
M.W : 429.25
SMILES Code : O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN
Synonyms :
GSK2141795; GSK795
MDL No. :MFCD28144686
InChI Key :AXTAPYRUEKNRBA-JTQLQIEISA-N
Pubchem ID :51042438

Safety of Uprosertib

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

Related Pathways of Uprosertib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • Akt3

    Akt3, IC50:38 nM

  • Akt1

    Akt1, IC50:180 nM

  • Akt2

    Akt2, IC50:328 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HAP1 cells 10 µM 48 hours To evaluate the effect of FDA-approved drugs on cell viability, Uprosertib showed high inhibitory activity PMC8210561
MKN45 cells 5 µM To evaluate the effect of Uprosertib on cell apoptosis, Uprosertib showed induced apoptosis ability PMC8210561
Human umbilical vein endothelial cells (HUVECs) 10 μM 30 minutes Uprosertib inhibited senkyunolide A and scopoletin-induced eNOS phosphorylation, indicating that senkyunolide A and scopoletin trigger endothelium-dependent vasodilation via the activation of the Akt-eNOS-NO signaling pathway. PMC10206061

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c-nu/nu mice MKN45 xenograft model Oral 10 mg/kg/day Once daily for 3 weeks To evaluate the inhibitory effect of Uprosertib on tumor growth, Uprosertib significantly inhibited tumor growth PMC8210561

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00920257 Cancer PHASE1 COMPLETED 2013-04-17 GSK Investigational Site, Balt... More >>imore, Maryland, 21231-2410, United States|GSK Investigational Site, Boston, Massachusetts, 02115, United States|GSK Investigational Site, New York, New York, 10021, United States|GSK Investigational Site, Oklahoma City, Oklahoma, 73104, United States|GSK Investigational Site, Nashville, Tennessee, 37203, United States|GSK Investigational Site, Houston, Texas, 77030, United States|GSK Investigational Site, Toronto, Ontario, M5G 2M9, Canada Less <<
NCT01266954 Solid Tumours PHASE1 COMPLETED 2011-09-01 GSK Investigational Site, Lond... More >>on, W12 0HS, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.65mL

2.33mL

1.16mL

23.30mL

4.66mL

2.33mL

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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