PI3K-IN-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PI3K-IN-2 

PI3K-IN-2 (compound 10) 是一种口服有效的 PI3Kβ/δ 抑制剂 (IC50=7.1/8.6 nM),与 PI3Kσ、PI3Kγ 相比 (IC50=13/190 nM),选择性更好。

PI3K-IN-2

PI3K-IN-2 Chemical Structure

CAS No. : 1403458-28-5

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生物活性

PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1].

IC50 & Target

PI3Kα

13 nM (IC50)

PI3Kβ

7.1 nM (IC50)

PI3Kδ

190 nM (IC50)

PI3Kγ

8.6 nM (IC50)

体外研究
(In Vitro)

PI3K-IN-2 (compound 10) shows PI3Kβ cell IC50 1.1 nM in phosphatase and tensin homolog (PTEN) null MDA-MB-468 cell and PI3Kδ cell IC50 14 nM in Jeko-1 B-cell[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

525.54

Formula

C28H29F2N3O5

CAS 号

1403458-28-5

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.

参考文献
  • [1]. Barlaam B, et al. Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954.

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