2. PI3K/Akt/mTOR Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. PI3K mTOR Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism Bcl-2 Family Caspase
  4. PI3K/mTOR-IN-22

PI3K/mTOR-IN-22 是一种具有口服活性的 PI3K/mTOR 激酶双重抑制剂，其 IC50 值分别为 400.5 nM 和 8.2 nM。PI3K/mTOR-IN-22 可下调 AKT 和 mTOR 的磷酸化水平，上调促凋亡蛋白 Bax 和 caspase-3，同时下调抗凋亡蛋白 Bcl-2。PI3K/mTOR-IN-22 对癌细胞具有抗增殖活性，可诱导细胞凋亡 (apoptosis) 和活性氧 (ROS) 产生，并降低线粒体膜电位。PI3K/mTOR-IN-22 在乳腺癌小鼠模型中表现出抗肿瘤活性。

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PI3K/mTOR-IN-22

PI3K/mTOR-IN-22 Chemical Structure

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PI3K/mTOR-IN-22 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models[1].

IC50 & Target[1]

Bax

 

Bcl-2

 

Caspase 3

 

体外研究
(In Vitro)

PI3K/mTOR-IN-22 (Compound J-33) 是一种 PI3K 和 mTOR 激酶的选择性双重抑制剂，对 PI3Kα 的 IC50 为 400.5 nM，对 mTOR 的 IC50 为 8.2 nM，可与两种激酶形成稳定的结合相互作用[1]。
PI3K/mTOR-IN-22 可强效抑制人乳腺癌 MCF-7 细胞的增殖，其 IC50 为 1.5 μM，同时还可抑制 H1975、H460、PC-9 细胞的增殖，IC50 值为 0.7、2.3 以及 13.5 μM[1]。
PI3K/mTOR-IN-22 (256 μg/mL) 在绵羊红细胞中表现出较低的溶血毒性，溶血率为 2.60%[1]。
PI3K/mTOR-IN-22 (0.75-1.50 μM; 6-12 h) 可诱导人乳腺癌 MCF-7 细胞发生浓度依赖性凋亡，降低线粒体膜电位，并升 ROS 水平[1]。
PI3K/mTOR-IN-22 (0.75-1.50 μM; 24 h) 可通过划痕愈合实验在体外呈剂量依赖性抑制人乳腺癌 MCF-7 细胞的迁移[1]。
PI3K/mTOR-IN-22 (0.19-3.00 μM; 14 days) 可剂量依赖性地抑制人乳腺癌 MCF-7 细胞的克隆形成能力[1]。
PI3K/mTOR-IN-22 (0.75-6.00 μM) 可剂量依赖性地下调人乳腺癌 MCF-7 细胞中 AKT 和 mTOR 的磷酸化水平，从而抑制 PI3K-AKT-mTOR 信号通路[1]。

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

PI3K/mTOR-IN-22 相关抗体:

Cell Migration Assay [1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0.75, 1.50 μM
Incubation Time: 24 h
Result: Significantly reduced the wound healing rate in cells treated with 0.75 μM relative to the control group.
Significantly reduced the wound healing rate in cells treated with 1.50 μM relative to the control group.
Showed an inhibitory effect that increased with concentration.

Immunofluorescence[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0.75, 1.50 μM
Incubation Time: 6-12 h
Result: Increased AO red/green fluorescence ratio.
Increased JC-1 red/green fluorescence ratio.
Increased DCFH-DA fluorescence intensity.
体内研究
(In Vivo)

PI3K/mTOR-IN-22 (Compound J-33) (75 mg/kg；口服；隔日一次；共 23 天) 在携带 MCF-7 异种移植物的 BALB/c 裸鼠中展现出强效的体内抗肿瘤活性，肿瘤抑制率达 44.9%[1]。

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

Animal Model: Breast cancer BALB/c nude (female, 4-6 weeks old, athymic injected with MCF-7 cells)[1]
Dosage: 75 mg/kg
Administration: p.o.; every other day; 23 days
Result: Achieved a tumor inhibition rate of 44.9%.
Significantly reduced phosphorylation of AKT at Ser473 and mTOR in tumor tissue.
Blocked the PI3K-AKT-mTOR signaling pathway.
Upregulated pro-apoptotic proteins Bax and Caspase-3.
Downregulated anti-apoptotic protein Bcl-2 and proliferation marker Ki-67.
Induced tumor cell apoptosis (evidenced by increased TUNEL-positive cells).
Caused no significant organ damage via H&E staining of mouse tissues.
分子量

610.68

Formula

C28H34N8O6S
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-22 相关分类

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  • 稀释计算器

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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-22PI3KmTORAktApoptosisReactive Oxygen Species (ROS)Mitochondrial MetabolismBcl-2 FamilyCaspasePhosphoinositide 3-kinaseMammalian target of RapamycinPKBProtein kinase Bbreast cancerMCF-7 human breast cancer cellsH1975 human lung cancer cellsapoptosisH460 human lung cancer cellssheep erythrocytesBALB/c nude micePI3K-AKT-mTOR pathwayInhibitorinhibitorinhibit

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