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Chemical Structure| 1227911-45-6 Chemical Structure| 1227911-45-6

Structure of GSK2334470
CAS No.: 1227911-45-6

Chemical Structure| 1227911-45-6

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GSK2334470 is a PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

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Product Details of GSK2334470

CAS No. :1227911-45-6
Formula : C25H34N8O
M.W : 462.59
SMILES Code : O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5
MDL No. :MFCD21608525
InChI Key :QLPHOXTXAKOFMU-WBVHZDCISA-N
Pubchem ID :46215815

Safety of GSK2334470

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GSK2334470

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • PDK1

    PDK-1, IC50:10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
CD4 T cells 2.5 mM 3 days GSK significantly attenuated HS-induced phosphorylation of PDPK1 and SGK1, and corrected the Th17 enhancement and Treg impediment triggered by HS iScience. 2024 Apr 26;27(6):109798.
CD4 T cells 5 mM, 10 mM 3 days GSK significantly increased CD4 T cell apoptosis and inhibited their proliferation iScience. 2024 Apr 26;27(6):109798.
ER+ breast cancer cell lines 1 µM 72 hours To synergistically inhibit proliferation and increase apoptosis Cancer Res. 2017 May 1;77(9):2488-2499.
LAN-1-MK cells 5 µM 72 hours GSK2334470 significantly inhibited the growth of LAN-1-MK cells and induced G0-G1 phase cell accumulation. Cancer Cell Int. 2015 Sep 29;15:91.
KP-N-SIFA-MK cells 5 µM 72 hours GSK2334470 significantly inhibited the growth of KP-N-SIFA-MK cells and induced G0-G1 phase cell accumulation. Cancer Cell Int. 2015 Sep 29;15:91.
SK-N-DZ-MK cells 5 µM 72 hours GSK2334470 significantly inhibited the growth of SK-N-DZ-MK cells and induced G0-G1 phase cell accumulation. Cancer Cell Int. 2015 Sep 29;15:91.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MCF-7 xenograft model Intraperitoneal injection 100 mg/kg Three times per week for 6 weeks To determine the efficacy in decreasing tumor growth Cancer Res. 2017 May 1;77(9):2488-2499.
DBA/1 mice Collagen-induced arthritis model Intraperitoneal injection 25 mg/kg Every three days for 21 days GSK significantly alleviated HS diet-exacerbated arthritis symptoms and corrected the Th17/Treg imbalance iScience. 2024 Apr 26;27(6):109798.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.81mL

2.16mL

1.08mL

21.62mL

4.32mL

2.16mL

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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