Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,130 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,720 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 753 | 现货 |
产品描述 | CZ415 is a potent and highly selective mTOR inhibitor. |
靶点活性 | mTOR:8.07(pIC50) |
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]. |
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) |
分子量 | 459.56 |
分子式 | C22H29N5O4S |
CAS No. | 1429639-50-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (182.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.176 mL | 10.88 mL | 21.7599 mL | 54.3999 mL |
5 mM | 0.4352 mL | 2.176 mL | 4.352 mL | 10.88 mL | |
10 mM | 0.2176 mL | 1.088 mL | 2.176 mL | 5.44 mL | |
20 mM | 0.1088 mL | 0.544 mL | 1.088 mL | 2.72 mL | |
50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.088 mL | |
100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.544 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CZ415 1429639-50-8 PI3K/Akt/mTOR signaling mTOR inhibit Inhibitor CZ-415 Mammalian target of Rapamycin CZ 415 inhibitor