2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. PI-540

PI-540 是双环噻吩并嘧啶衍生物，是口服有效的 PI3K 抑制剂。PI-540 具有抗癌细胞增殖和高组织分布度的特性。PI-540 可抑制 PI3K 不同亚型，IC50s 分别为 10 nM (P110α)，3510 nM (P110β)，410 nM (P110δ)，33110 nM (P110γ)。PI-540 还抑制 mTOR (IC50: 61 nM) 和 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 相关抗体

Top Publications Citing Use of Products

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
细胞效力
(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]
分子量

425.55

Formula

C22H27N5O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PI-540 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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目录号：
HY-10116
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