2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Cytoskeleton
  3. PI3K mTOR Akt CDK Cadherin
  4. PI3Kα-IN-29

PI3Kα-IN-29 是一种高效的、口服有效且选择性的 PI3Kα 抑制剂，IC50 值为 2.5 nM。PI3Kα-IN-29 对 PI3Kβ/δ/γ/mTOR 的选择性超过 400 倍。PI3Kα-IN-29 可选择性降解 H1047R 突变型 p110α 蛋白，并抑制 PI3Kα 激酶活性。PI3Kα-IN-29 可抑制 PI3K/AKT/mTOR 信号通路，诱导 G1 期阻滞，并抑制细胞迁移。PI3Kα-IN-29 可抑制 T47 小鼠模型中的肿瘤生长。PI3Kα-IN-29 可用于乳腺癌的研究。

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PI3Kα-IN-29

PI3Kα-IN-29 Chemical Structure

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PI3Kα-IN-29 相关抗体

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

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Akt Akt1 Akt2 Akt3

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer[1].

IC50 & TargetHY-179623

PI3Kα

2.5 nM (IC50)

PI3Kβ

>1000 nM (IC50)

PI3Kδ

>1000 nM (IC50)

PI3Kγ

>1000 nM (IC50)

体外研究
(In Vitro)

PI3Kα-IN-29 (compound A32) (72 小时) 在 T47D 和 MCF7 细胞中表现出强效的抗增殖活性，IC50 分别为 0.157 和 0.373 μM[1]。
PI3Kα-IN-29 (0-5 μM，0-24 小时) 剂量依赖性地诱导 T47D 和 MCF7 细胞的 G1 期阻滞，并通过抑制 PI3K/AKT/mTOR 通路抑制细胞迁移[1]。
A32 (0.1-5 μM，24 小时) 抑制 PI3K/AKT/mTOR 信号传导，并诱导 T47D 细胞中突变 p110α (PI3Kα 的催化亚基) 的降解[1].
PI3Kα-IN-29 与 Val851 形成关键的氢键，并与 Gln859 和 Ser854 形成三方氢键网络，而苯并恶唑部分与 Lys802、Ser774 和 Ala775 相互作用，从而导致强效的 PI3Kα 抑制[1]。
PI3Kα-IN-29 (125 nM-2 μM，14 天) 以浓度依赖的方式抑制 MCF7 细胞的集落形成[1]。

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

PI3Kα-IN-29 相关抗体:

Cell Cycle Analysis[1]

Cell Line: T47D, MCF7
Concentration: T47D: 0, 100, 500 nM
MCF7: 0, 1.25, 5 µM
Incubation Time: 24 h
Result: Concentration-dependently induced G1 phase arrest both in T47D and MCF7 celss.
Increased G1 population to 71.8% and 60.2% in T47D at 500 and 100 nM, respectively.
In MCF7 cells, a similar G1 arrest pattern was observed at 1.25 and 5 µM.

Western Blot Analysis[1]

Cell Line: T47D, RKO, HCT116, SKOV3, SKBR3, PC3, MCF10A and MCF7
Concentration: 0, 0.5, 1, 5 μM
Incubation Time: 24 h
Result: Concentration-dependently suppressed phosphorylation of AKT (Ser473) in all tested cell lines.
Selectively induced degradation of mutant PI3Kα protein (H1047R) in a concentration-dependent manner, with the most pronounced effect in T47D cells.\r
Significant degradation was also observed in other PIK3CA-mutant lines: RKO, HCT116 (colorectal cancer), and SKOV3 (ovarian cancer).
No degradation was observed in wild-type (SKBR3, MCF10A) or E545K-mutant (MCF7) cell lines.

Cell Migration Assay [1]

Cell Line: MCF7
Concentration: 125, 250, 500 nM
Incubation Time: 0, 12, 24 h
Result: Significantly suppressed MCF7 cell migration, with minimal wound closure observed even at low concentrations after 24 h.

Western Blot Analysis[1]

Cell Line: T47D, MCF7
Concentration: 0, 0.1, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Upregulated p27 expression, and downregulated E-cadherin expression.
Demonstrated concentration-dependent suppression of retino-blastoma (RB) protein phosphorylation, with concomitant RB degradation observed at higher concentrations.

Cell Proliferation Assay[1]

Cell Line: MCF7
Concentration: 125, 250, 500 nM, 1 and 2 μM
Incubation Time: 14 days
Result: Concentration-dependently inhibited colony formation in MCF7 cells.
Achieved near‑complete suppression at higher concentrations (≥1 µM).
体内研究
(In Vivo)

PI3Kα-IN-29 (50 和 100 mg/kg，口服，每日一次，持续 21 天) 在 T47D 异种移植小鼠模型中表现出强大的体内抗肿瘤功效以及良好的安全性[1]。
PI3Kα-IN-29 (500、1000 和 1500 mg/kg，灌胃，单次给药) 在 ICR 小鼠中表现出良好的安全性[1]。

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

Animal Model: BALB/c nude mice subcutaneously inoculated with T47D cells[1]
Dosage: 50 and 100 mg/kg
Administration: p.o., once daily for 21 days
Result: Achieved 70.7% and 52.3% tumor growth inhibition (TGI) at 100 and 50 mg/kg, respectively.
Showed a marked tumor regression at 100 mg/kg.
Showed no significant changes in body weight and no apparent histopatho-logical abnormalities.
Dose-dependently reduced Ki67 expression and phosphorylation of AKT.
Animal Model: ICR mice[1]
Dosage: 500, 1000, and 1500 mg/kg
Administration: i.g., single dose
Result: Revealed no significant body weight loss roup throughout the 14-day period.
Showed no inflammatory infiltration or organ-specific lesions in all major organs.
分子量

391.38

Formula

C20H17N5O4
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

PI3Kα-IN-29 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:

PI3Kα-IN-29PI3KmTORAktCDKCadherinPhosphoinositide 3-kinaseMammalian target of RapamycinPKBProtein kinase BCyclin dependent kinaseMCF7migration inhibitionalpelisibH1047R mutant p110αhyperglycemiaPI3Kα IC50tumor growth inhibitionT47DpharmacokineticsPI3KαPI3Kα-selective inhibitorG1 arrestInhibitorinhibitorinhibit

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