2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. 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).

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PI-540 Chemical Structure

PI-540 Chemical Structure

CAS No. : 885616-78-4

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PI-540 Related Antibodies

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mTOR mTORC1 mTORC2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

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)[1].

IC50 & Target

IC50: 10 nM (P110α)，3510 nM (P110β)，410 nM (P110δ)，33110 nM (P110γ)[1]br/IC50: 61 nM (mTOR), 525 nM (DNA-PK)[1]
Cellular Effect
Cell Line Type Value Description References
A2780 IC50
0.16 μM
Compound: 8
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
[PMID: 18754654]
Sf9 IC50
0.01 μM
Compound: 8
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
[PMID: 18754654]
U-87MG ATCC IC50
1.01 μM
Compound: 8
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
[PMID: 18754654]
Molecular Weight

425.55

Formula

C22H27N5O2S
CAS No.
SMILES

OC1=CC=CC(C2=NC(N3CCOCC3)=C(SC(CN4CCN(C)CC4)=C5)C5=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PI-540 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI-540885616-78-4PI540PI 540mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaseBicyclic thienopyrimidineoral effectivehigh tissue distributionanti-proliferativeInhibitorinhibitorinhibit

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HY-10116
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