PI3K-IN-22

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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-22 

PI3K-IN-22 是一种 PI3Kα/mTOR 双重激酶抑制剂。PI3K-IN-22 对 PI3Kα 和 mTOR 的 IC50s 值分别为 0.9、0.6 nM。PI3K-IN-22 可用于癌症研究。

PI3K-IN-22

PI3K-IN-22 Chemical Structure

CAS No. : 1202884-94-3

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生物活性

PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer[1].

IC50 & Target[1]

PI3Kα

0.9 nM (IC50)

mTOR

0.6 nM (IC50)

体外研究
(In Vitro)

PI3K-IN-22 (compound 46) inhibits the cell growth of PC3 and MDA-361 cells with IC50s of <3.0 and 13.0 nM[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-22 (25 mg/kg; i.v.) suppresses phosphorylation of Akt T308, Akt S473 and S6K in MDA361 breast tumor cells up to 8 h in MDA361 tumor bearing nude mice demonstrated by biomarker studies[1].
PI3K-IN-22 (50, 25, 10 mg/kg; i.v.; once daily for 5 days weekly; 2 rounds) shows good antitumor efficacy in MDA361 tumor xenograft nude mice model[1].
PI3K-IN-22 (25 mg/kg; i.v.; a single dose) has a blood concentrationsat value of 1731 ng/mL at 8 h[1].

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

Animal Model: MDA361 tumor xenograft nude mice model[1]
Dosage: 50, 25, 10 mg/kg
Administration: i.v., once daily for 5 days weekly (2 rounds)
Result: Exhibited significant tumor regression in 50 mg/kg and no tumor regrowth until day 32.
Exhibited tumor growth inhibition in 25 and 10 mg/kg.

分子量

624.66

Formula

C31H35F3N8O3
CAS 号

1202884-94-3
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]. Chen Z, et al. Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. J Med Chem. 2010 Apr 22;53(8):3169-82.

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