PF-5177624
PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 1350821-45-2
- Formula: C25H25FN8O2
- Molecular Weight:488.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
1800 nM
Compound: 24
|
Antiproliferative activity against human A549 cells after 72 hrs by resazurin reduction assay
Antiproliferative activity against human A549 cells after 72 hrs by resazurin reduction assay
|
[PMID: 22040023] |
| A549 | IC50 |
50 nM
Compound: 24
|
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human A549 cells after 2 hrs by ELISA
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human A549 cells after 2 hrs by ELISA
|
[PMID: 22040023] |
| NCI-H460 | EC50 |
700 nM
Compound: 24
|
Antiproliferative activity against human H460 cells after 72 hrs by resazurin reduction assay
Antiproliferative activity against human H460 cells after 72 hrs by resazurin reduction assay
|
[PMID: 22040023] |
| SK-OV-3 | IC50 |
70 nM
Compound: 24
|
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human SKOV3 cells after 2 hrs by ELISA
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human SKOV3 cells after 2 hrs by ELISA
|
[PMID: 22040023] |
Chemical Information
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CAS No. 1350821-45-2
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Molecular Weight 488.52
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Formula C25H25FN8O2
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SMILES
O=CN1[C@@H]([C@@H](CC1)NC2=NC(C(C3=CN(C4=NC=NC(N)=C43)C(C)C)=O)=CN=C2)C5=CC=C(C=C5)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)