1. PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  2. Akt Ribosomal S6 Kinase (RSK) GSK-3
  3. XL-418

XL-418 是一种口服有效的双重 Aktp70S6K 抑制剂,其 IC50 值分别为 1 nM 和 2 nM。XL-418 可抑制核糖体蛋白 S6 和 GSK3β 的磷酸化。XL-418 可用于前列腺癌和乳腺癌的研究。

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XL-418

XL-418 Chemical Structure

CAS No. : 871343-09-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XL-418 is an orally active dual Akt and p70S6K inhibitor with IC50s of 1 nM for Akt1 and 2 nM for p70S6K. XL-418 inhibits the phosphorylation of ribosomal protein S6 and GSK3β. XL-418 can be used for the study of prostate carcinoma and breast cancer[1].

IC50 & Target[1]

Akt1

1 nM (IC50)

p70S6K

2 nM (IC50)

GSK-3β

 

体外研究
(In Vitro)

XL-418 抑制核糖体蛋白 S6 的磷酸化,在 A549 和 PC-3 细胞中的 IC50 值分别为 30 nM 和 55 nM。XL-418 抑制 GSK3β 的磷酸化,在 PC-3 细胞中的 IC50 值为 194 nM[1]

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

体内研究
(In Vivo)

XL-418 (compound 11b;100 mg/kg;口服;每日两次;共五次给药) 可抑制 PC-3 前列腺癌模型中核糖体蛋白 S6 和 GSK3β 的磷酸化[1]
XL-418 (50 mg/kg;口服;每日一次;连续 15 天) 可抑制 PC-3 前列腺癌模型中的肿瘤生长[1]
XL-418 (50-100 mg/kg;口服;每 4 天给药两天) 在本研究中显示出高度活性,50 mg/kg 剂量组的肿瘤生长抑制率为 71%,100 mg/kg 交替给药方案组的肿瘤生长抑制率 (TGI) 为 96%[1]

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

分子量

609.48

Formula

C26H32BrF3N8O

CAS 号
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
  • 摩尔计算器

  • 稀释计算器

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

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