化合物CZ415 T3514

Product Introduction
Bioactivity


英文名: CZ415

描述: CZ415 是高选择性的mTOR 抑制剂，其 pIC50=8.07。它对mTORC1和mTORC2复合体具有抑制作用。

细胞实验: Cells are seeded in 90 μL DMEM containing 2% FCS at 4x104 cells/well (for pS6RP S240/244 assay) or 8x104 cells/well (for pAKT S473 assay) in a 96well U-bottom plate. The plate is then incubated for 1h in a humidified incubator (37oC, 5% CO2) to allow cells to adhere. CZ415: 3 μM start, 8 points 1:3 dilution steps, n=2. Positive control: 1 μM PI-103 (n=8). Negative control: DMSO (n=8). 10 μL of 10x compound concentration in 1% DMSO/99% (DMEM 2% FCS) are added to the cells followed by 2 h incubation in a humidified incubator (37oC, 5% CO2). Cells are lysed by addition of 10 μL 5x Complete Lysis Buffer and gentle shaking at 4°C for 15 min (Only for Reference)

体外活性: CZ415 shows no genotoxic potential and has very good cell permeability. Treatment of CZ415 leads to inhibition of phosphorylation for downstream targets of mTORC1 and mTORC2(IC50=14.5 nM for pS6RP and IC50=14.8 nM for pAKT). The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 h in stimulated human whole blood, and the resulting IC50 was 226 nM. CZ415 shows no genotoxic potential. It is neither mutagenic in a bacterial mutation assay (Ames test) nor does it show genotoxicity in the mouse lymphoma assay (MLA), in either the presence or absence of rat-liver S9 mix[1].

体内活性: In vivo studies show that CZ415 has moderate clearance and good oral bioavailability. In an anti-CD3 mouse model CZ415 efficiently inhibits mTOR downstream signaling and, in a CIA mouse model, shows significant antiinflammatory effects. With its extraordinary selectivity, drug-like properties and proven efficacy in vivo, CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 84 mg/mL (182.8 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Inhibitor | CZ415 | mTOR | CZ-415 | Mammalian target of Rapamycin | CZ 415

相关产品: Apitolisib | PI3Kα/mTOR-IN-1 | Chromeceptin | SF2523 | Pictilisib dimethanesulfonate | mTOR inhibitor-12 | XL388 | Kazinol A | Torin 1 | D-α-Hydroxyglutaric acid disodium

相关库: Anti-Aging Compound Library | Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | Highly Selective Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Autophagy Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途