2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. PI3Kα-IN-30

PI3Kα-IN-30 是一种口服有效的、选择性的 PI3Kα 抑制剂，其 IC50 为 2.8 nM。PI3Kα-IN-30 可抑制癌细胞增殖，并抑制 Akt (S473) 和 pS6 (S240/244) 的磷酸化。PI3Kα-IN-30 在 30 μM 浓度下对正常体细胞系的生长抑制活性较低。PI3Kα-IN-30 可诱导癌细胞凋亡且在异种移植模型中发挥抗肿瘤功效。PI3Kα-IN-30 可用于乳腺癌的研究。

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PI3Kα-IN-30

PI3Kα-IN-30 Chemical Structure

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PI3Kα-IN-30 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

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC50 of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer[1].

IC50 & Target[1]

PI3K alpha

2.8 nM (IC50)

体外研究
(In Vitro)

PI3Kα-IN-30 (Compound 26) (0.001-30 μM; 72 h) 可强效抑制 T47D、MCF-7 和 HCC1954 人乳腺癌细胞系的增殖，其中对 T47D 细胞的活性最强 (IC50 = 0.0084 μM)[1]。
PI3Kα-IN-30 (30 μM) 在 30 μM 浓度下对正常体细胞 HK-2、LX-2 和 BEAS-2B 仅表现出极微弱的生长抑制作用[1]。
PI3Kα-IN-30 (0.03-3 μM; 1 h) 可通过降低 Akt 和 S6 的磷酸化水平，以剂量依赖方式下调 T47D 细胞中的 PI3K 信号通路[1]。
PI3Kα-IN-30 (1 μM; 48 h) 可在 1 μM 浓度、处理 48 h 后诱导 T47D 细胞发生凋亡[1]。

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

PI3Kα-IN-30 相关抗体:

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 1 h
Result: Dose-dependently reduced the phosphorylation level of Akt (S473) and S6 (S240/244) in T47D cells.
Showed significant inhibition at concentrations as low as 0.03 μM for pAkt(S473) and 0.1 μM for pS6(S240/244).

Apoptosis Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced apoptosis in T47D cells at 1 μM, with statistical significance compared to controls.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 CL AUC0-t AUC0-∞ Vz MRT0-t MRT0-∞ F
Rat[1] 1 mg/kg i.v. 2013 ng/mL 0.033 h 0.51 h 1035 mL/h/kg 2426 ng·h/mL 973 ng·h/mL 761 mL/kg 0.55 h 0.57 h /
Rat[1] 10 mg/kg p.o. 1443 ng/mL 0.51 h 3.00 h 3345 mL/h/kg 3238 ng·h/mL 3405 ng·h/mL 15142 mL/kg 2.20 h 2.77 h 34.8 %
Mice[1] 3.4 mg/kg i.v. 3323 ng/mL 0.083 h 3.11 h 768 mL/h/kg 4502 ng·h/mL 4530 ng·h/mL 3338 mL/kg 1.48 h 1.61 h /
Mice[1] 15 mg/kg p.o. 1940 ng/mL 2.67 h 2.61 h 1277 mL/h/kg 11375 ng·h/mL 12220 ng·h/mL 4749 mL/kg 3.99 h 4.46 h 61.1 %
体内研究
(In Vivo)

PI3Kα-IN-30 (Compound 26) (20-40 mg/kg; p.o.; 每日一次共 21 天) 在携带PIK3CA突变的 HCC1954 乳腺癌移植瘤小鼠模型中有效抑制肿瘤生长[1]。

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

Animal Model: BALB/c-Nude (6-8 weeks old, 20 females) mice[1]
Dosage: 20 and 40 mg/kg
Administration: p.o.; once daily for 21 consecutive days
Result: Achieved a tumor growth inhibition rate (TGI) of 71.98% at 40 mg/kg.
分子量

575.61

Formula

C26H28F3N7O3S
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-30 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 *
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The dilution calculator equation

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

PI3Kα-IN-30PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase Bbreast cancerHCC1954PI3KδT47DPI3KαpS6MCF-7PI3KγPI3KβInhibitorinhibitorinhibit

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目录号：
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