2. PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. PI3K mTOR Apoptosis Bcl-2 Family MDM-2/p53 Telomerase Mitochondrial Metabolism
  4. PI3K/mTOR-IN-19

PI3K/mTOR-IN-19 是一种口服有效的强效选择性 PI3K (IC50 = 4.23 nM) 和 mTOR (IC50 = 2.3 nM) 抑制剂。PI3K/mTOR-IN-19 可显著抑制 Eca109 细胞的活力并诱导细胞凋亡 (apoptosis)。PI3K/mTOR-IN-19 可导致 G0/G1 期细胞周期阻滞、线粒体膜 (mitochondrial membrane) 电位降低，并表现出显著的端粒酶 (telomerase) 抑制活性。PI3K/mTOR-IN-19 可调节关键凋亡调节因子 (Bcl-2、Bax 和 p53) 的表达，并下调 PI3K/Akt/mTOR 信号通路。PI3K/mTOR-IN-19 可用于食管癌的研究。

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PI3K/mTOR-IN-19

PI3K/mTOR-IN-19 Chemical Structure

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Customer Review

PI3K/mTOR-IN-19 相关抗体

Top Publications Citing Use of Products

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

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/mTOR-IN-19 is an orally active, potent, selective PI3K (IC50 = 4.23 nM) and mTOR (IC50 = 2.3 nM) inhibitor. PI3K/mTOR-IN-19 significantly inhibits Eca109 cell viability and induces apoptosis. PI3K/mTOR-IN-19 causes G0/G1 cell cycle arrest, decreased mitochondrial membrane potential, and demonstrates marked telomerase inhibitory activity. PI3K/mTOR-IN-19 modulates the expression of key apoptotic regulators (Bcl-2, Bax, and p53) and downregulates the PI3K/Akt/mTOR signaling pathway. PI3K/mTOR-IN-19 can be used for the study of esophageal cancer[1].

IC50 & Target

PI3K

4.23 nM (IC50)

mTOR

2.3 nM (IC50)

Bax

 

Bcl-2

 

体外研究
(In Vitro)

PI3K/mTOR-IN-19 (Compound 8e) (2.5-10 μM，48-72 小时) 对多种癌细胞系表现出最显著的抑制活性，尤其对多种食管鳞状细胞癌 (ESCC) 细胞系具有显著的抑制作用，对非肿瘤性上皮细胞的细胞毒性极低，并呈剂量依赖性地抑制 Eca109 细胞增殖，同时诱导细胞毒性形态学改变[1]。
PI3K/mTOR-IN-19 (2.5-10 μM，24 小时) 可诱导 Eca109 细胞凋亡，抑制其迁移和侵袭能力，并增加 G0/G1 期细胞比例，同时降低 S 期和 G2 期细胞比例[1]。
PI3K/mTOR-IN-19 可抑制 Eca109 细胞端粒酶活性达 71.5%[1]。
PI3K/mTOR-IN-19 (2.5-10 μM，24 小时) 可降低线粒体膜电位 (ΔΨm)，表现为 Eca109 细胞中红/绿荧光比值的降低[1]。
PI3K/mTOR-IN-19 (2.5-10 μM) 可上调 Eca109 细胞中 p53 和 Bax 的表达，下调 Bcl-2 的表达；同时，它还能降低 p-PI3K、p-Akt (Ser473) 和 p-mTOR 的水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PI3K/mTOR-IN-19 相关抗体:

Cell Proliferation Assay[1].

Cell Line: HeLa cells, MCF-7 cells, HepG-2 cells, A549 cells, Eca109 cells, MCF12A cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Cervical cancer (HeLa, IC50 = 23.12 µM)
Human breast cancer cell line (MCF-7, IC50 = 22.03 µM)
Liver cancer cell line (HepG-2, IC50 = 16.72 µM)
Lung cancer cell line (A549, IC50 = 17.78 µM)
Esophageal cancer (Eca109, IC50 = 0.28 µM)
Non-tumorigenic epithelial cell (MCF12A, IC50 ＞ 250 µM)

Cell Proliferation Assay[1].

Cell Line: TE1, TE13, KYSE30, KYSE70, KYSE150
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: TE1 (IC50 = 1.34 μM) TE13 (IC50 = 2.78 μM) KYSE30 (IC50 = 1.23 μM) KYSE70 (IC50 = 1.11 μM) KYSE150 (IC50 = 1.05 μM)

Apoptosis Analysis[1].

Cell Line: Eca109 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Significantly increased proportion of Annexin V/PI positive cells indicates an increase in early and late apoptotic cells.
体内研究
(In Vivo)

PI3K/mTOR-IN-19 (Compound 8e) (2-5 mg/kg，腹腔注射，每周 3 次，持续 14 天) 在 Eca109 细胞荷瘤小鼠中表现出剂量依赖性的肿瘤生长抑制作用，且未观察到明显的毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A subcutaneous injection of 1×106 Eca109 cells with Matrigel at a dilution of 1:1 was administered to the right flank region of every single male BALB/c null nude mice (6-week-old)[1].
Dosage: 2 mg/kg, 5 mg/kg, 10 mg/kg
Administration: I.p., 3 times a week for 14 days
Result: MDA levels were decreased, while SOD and GSH activities were increased.
The expression of TNF-α, IL-1β, and IL-6 was significantly inhibited.
The expression of PI3K and p-Akt (Ser473) proteins in tumor tissues was significantly reduced.
分子量

465.52

Formula

C25H28FN5O3
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

PI3K/mTOR-IN-19 相关分类

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  • 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:

PI3K/mTOR-IN-19PI3KmTORApoptosisBcl-2 FamilyMDM-2/p53TelomeraseMitochondrial MetabolismPhosphoinositide 3-kinaseMammalian target of Rapamycincell cycleoxidative stresscytokinespharmacokineticsInhibitorinhibitorinhibit

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