PI-540
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM).
For research use only. We do not sell to patients.
- CAS No.: 885616-78-4
- Formula: C22H27N5O2S
- Molecular Weight:425.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 10 nM (P110α)，3510 nM (P110β)，410 nM (P110δ)，33110 nM (P110γ)[1]br/IC50: 61 nM (mTOR), 525 nM (DNA-PK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.16 μM
Compound: 8
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Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay
Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay
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[PMID: 18754654] |
| Sf9 | IC50 |
0.01 μM
Compound: 8
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Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
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[PMID: 18754654] |
| U-87MG ATCC | IC50 |
1.01 μM
Compound: 8
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Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay
Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay
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[PMID: 18754654] |
Chemical Information
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CAS No. 885616-78-4
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Molecular Weight 425.55
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Formula C22H27N5O2S
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SMILES
OC1=CC=CC(C2=NC(N3CCOCC3)=C(SC(CN4CCN(C)CC4)=C5)C5=N2)=C1
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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)
PI-540 Related Classifications
HY-10116 Related Classifications
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