mTOR inhibitor-3

CAS: 1207358-59-5 货号: M654835 分子式: C25H30N8O2 分子量: 474.56 PubChem CID: 59239114
有货
级别和纯度: 10mM in DMSO
别名
mTOR抑制剂-3
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
M654835-1ml
期货 Stock Image
¥2,088.90
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为什么选择此级别

,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

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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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


mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a K i of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

In Vitro

mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a K i of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC 50 s of 150 nM and 57 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) . mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t 1/2 =1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal administration

Mice Human prostate cancer NCI-PC3 cells are implanted subcutaneously into the right hind flanks of female NCR nude mice (5×10 6 cells in 100 μL of Hank’s balanced salt solution). Tumors are monitored until they reach a mean tumor volume of approximately 500 mm 3 . Then similarly sized tumors are randomly assigned to groups (n=4). Compounds are formulated as suspensions in 0.5% methylcellulose/0.2% Tween 80 (MCT) and dosed orally at 25, 50, and 100 mg/kg (100 μL dose/25 g animal). Tumor and plasma samples are harvested at 1, 6, and 10 h postdose. aladdin has not independently confirmed the accuracy of these methods. They are for reference only.

规格

别名
mTOR抑制剂-3
规格或纯度
10mM in DMSO
英文名称
mTOR inhibitor-3
生化机理
在细胞和体内药代动力学(PK)/药效学(PD)实验中,mTOR 抑制剂-3 可抑制 mTORC1 和 mTORC2。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOC[C@@H]5C
PubChem CID
分子量
474.56

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常见问题

本产品应如何储存?
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输?
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 1207358-59-5,分子式为 C25H30N8O2,分子量为 474.56 g/mol。
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