2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. PI3K/mTOR-IN-20

PI3K/mTOR-IN-20 是一种选择性的双重 PI3K/mTOR 抑制剂。PI3K/mTOR-IN-20 在 MRC-5 和 Mlg2908 细胞中展现出纳摩尔级别的抗增殖效果其 IC50 值分别为 0.380 和 0.090 μM。在 Bleomycin 诱导的肺纤维化模型中，PI3K/mTOR-IN-20 能够降低 Ashcroft 评分、减少羟脯氨酸含量和胶原沉积，下调纤维化相关蛋白表达，并修复肺组织结构。PI3K/mTOR-IN-20 表现出良好的安全性，小鼠体重稳定恢复，且未出现明显的肝、肾毒性。PI3K/mTOR-IN-20 可用于肺成纤维细胞的相关研究。

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PI3K/mTOR-IN-20

PI3K/mTOR-IN-20 Chemical Structure

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Customer Review

PI3K/mTOR-IN-20 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

PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research[1].
IC50 & Target[1].

PI3Kα

 

PI3Kβ

 

PI3Kγ

 

PI3Kδ

 

PI3K

 

体外研究
(In Vitro)

PI3K/mTOR-IN-20 (compound 11) (处理 72 小时) 对 MRC-5 和 Mlg2908 细胞展现出纳摩尔级抗增殖活性，其 IC50值分别为 0.38 和 0.09 μM[1]。
PI3K/mTOR-IN-20 (1 μM) 可有效抑制 mTOR 及 I 类 PI3K 亚型 (α、β 和 γ)，同时对 PI3Kδ 的抑制活性较弱 (对 PI3Kα、PI3Kβ、PI3Kγ 和 mTOR 的抑制率分别为 94.89%、79.24%、42.60% 和 42.99%)[1]。
PI3K/mTOR-IN-20 (1 μM，处理 48 小时) 能有效抑制 MRC-5 细胞中的 PI3K 活性并减弱成纤维细胞活化[1]。

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

PI3K/mTOR-IN-20 相关抗体:

Western Blot Analysis[1]

Cell Line: MRC-5 cells
Concentration: 1 μM
Incubation Time: 48h
Result: Significantly reduced AKT phosphorylation (pAKT).
Suppressed the expression of key pulmonary fibrosis-associated proteins, fibroblast activation protein (FAP), fibronectin (FN), and α-smooth muscle actin (α-SMA).
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 2.5 mg/kg i.p. T1/2 0.79 h
Mice[1] 2.5 mg/kg i.v. T1/2 1.11 h
Mice[1] 2.5 mg/kg i.p. Cmax 449 ng/mL
Mice[1] 2.5 mg/kg i.v. CL 150 mL/min/kg
Mice[1] 2.5 mg/kg i.p. AUC0-∞ 315 ng·h/mL
Mice[1] 2.5 mg/kg i.v. Vss 3.7 L/kg
Mice[1] 2.5 mg/kg i.p. F 109 %
Mice[1] 2.5 mg/kg i.v. AUC0-∞ 290 h·ng/g
体内研究
(In Vivo)

PI3K/mTOR-IN-20 (compound 11) (15 mg/kg，腹腔注射，每日一次，持续 11 天) 在 Bleomycin (BLM) 诱导的肺纤维化小鼠模型中表现出强大的抗纤维化效应，可减轻胶原沉积、恢复肺组织结构、抑制促纤维化过程并改善生理指标，且安全性良好[1]。
PI3K/mTOR-IN-20 (15-60 mg/kg，腹腔注射，每日一次，持续 3 天) 在 Bleomycin (BLM) 诱导的肺纤维化小鼠模型中未表现出明显的肝毒性或肾毒性[1]。

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

Animal Model: Bleomycin (HY-108345A) (0.75 U/kg, i.p.) induced-male C57BL/6 mice (8-10 weeks)[1]
Dosage: 15 mg/kg
Administration: i.p., daily for 11 days
Result: Significantly attenuated the pathological changes, partially restoring normal lung structure and extensiving fibrotic remodeling[1].
Reduced Ashcroft scores, a quantitative measure of fibrosis severity[1].
Reversed the BLM-induced increase in the lung index (lung-to-body weight ratio), which reflects edema and fibrotic mass accumulation[1].
Robustly suppressed BLM-induced increase in d collagen deposition (a hallmark of fibrosis progression) [1].
Mitigated BLM-induced weight loss and maintained steady weight recovery[1].
Significantly inhibited fibroblast activation protein (FAP) expression[1].
Animal Model: ICR mice (8 weeks)[1]
Dosage: 15, 30, or 60 mg/kg
Administration: i.p., once daily for 3 days
Result: Revealed minimal toxicity in liver and kidney function[1].
Remained Serum levels of alanine transaminase (ALT) and aspartate transaminase (AST) within the normal range at doses of 15 and 30 mg/kg[1].
Unchanged serum creatinine (CREA) and uric acid (UA) levels (markers of kidney function) [1].
No Obvious structure changes occur in the livers[1].
分子量

618.61

Formula

C29H24F2N8O4S
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-20 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PI3K/mTOR-IN-20mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaseAshcroft scoresfetal lung fibroblastsInhibitorinhibitorinhibit

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