PI3K/mTOR Inhibitor-11

CAS: 2845104-25-6 货号: P651773 分子式: C27H21N7 分子量: 443.50
有货
级别和纯度: ≥98%
别名
PI3K/mTOR 抑制剂-11
储存条件
避光,-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
5mg
P651773-5mg
期货 Stock Image
¥5,400.90
10mg
P651773-10mg
期货 Stock Image
¥8,500.90
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为什么选择此级别

提供 ≥98% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

避光,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor ( IC 50 : 3.5, 4.6, and 21.3 nM for PI3Kα , PI3Kδ , and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers

In Vitro

PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC 50 values of 0.25, 0.17, 0.29, 0.09, 0.16, and 0.97 μM, respectively. PI3K/mTOR Inhibitor-11 (0-1.25 μM, 15 days) decreases the colony formation rates of HeLa and SW620 cells. PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) arrests HeLa and SW620 cells at the G0/G1 phases. PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) suppressees the phosphorylated AKT and S6 proteins in HeLa cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: HeLa and SW620 cells Concentration: 0, 0.15625, 0.625, 1.25 μM Incubation Time: 24 h Result: Affected HeLa cells’ apoptosis rate from 6.10 to 66.04% in a dose-dependent manner. Western Blot AnalysisCell Line: HeLa Concentration: 0, 0.15625, 0.625, 1.25, 2.5 μM Incubation Time: 24 h Result: Suppressed the phosphorylated AKT (Ser473 and Thr308) and S6 proteins.

In Vivo

PI3K/mTOR Inhibitor-11 (compound 8o, 15-60 mg/kg, intragastric administration) suppresses the growth of HeLa and SW620 xenograft tumors . PI3K/mTOR Inhibitor-11 (1 mg/kg for i.v., 10 mg/kg for p.o., rats) shows oral bioavailability (76.81%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: HeLa and SW620 xenograft models of female BALB/c nude mice . Dosage: 15, 30, and 60 mg/kg Administration: Intragastric administration, daily for 30 days. Result: The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively. TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively. Animal Model: Rats . Dosage: 1 mg/kg for i.v., 10 mg/kg for p.o. Administration: i.v., p.o. Result: Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o) dose (mg/kg) T 1/2 (h) C max (ng/mL) CL (mL/min/kg) F (%) 1 (i.v.) 17.2 10 (p.o.) 2.6 2995 76.81%

Form:Solid

IC50& Target:PI3Kα 3.5 nM (IC 50 ) PI3Kδ 4.6 nM (IC 50 ) mTOR 21.3 nM (IC 50 )

规格

别名
PI3K/mTOR 抑制剂-11
规格或纯度
≥98%
英文名称
PI3K/mTOR Inhibitor-11
生化机理
PI3K/mTOR Inhibitor-11 是一种口服活性 PI3K/mTOR 抑制剂(对 PI3Kα、PI3Kδ 和 mTOR 的 IC 50 分别为 3.5、4.6 和 21.3 nM)。PI3K/mTOR 抑制剂-11 通过抑制 AKT 和 S6 蛋白的磷酸化来调节 PI3K/AKT/mTOR 信号通路。PI
储存条件
避光,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
443.50

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高级数据

化学和物理性质
溶解性
DMSO : 40 mg/mL (90.19 mM; ultrasonic and warming and heat to 60°C)
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