Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NSC 405020 是一种 MT1-MMP 的非催化抑制剂,可特异地靶向 MT1-MMP 的 PEX 结构域,不会抑制 MT1-MMP 和 MMP-2的催化活性。
产品描述 | NSC 405020 is a noncatalytic inhibitor of MT1-MMP. |
体外活性 | NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP. NSC 405020 affects PEX homodimerization but not catalytic activity of MT1-MMP. NSC 405020 (100 μM) inhibits migration of cells with high level of MT1-MMP, with a reduction of migration efficiency by about 75%. NSC 405020 does not inhibit migration of cells with low level of MT1-MMP and does not inhibit cell adhesion on collagen.[1] |
体内活性 | NSC 405020 (0.5 mg/kg, intratumoral injection) significantly represses tumor growth. NSC 405020 causes a fibrotic, ΔPEX-like tumor phenotype and increases the level of COL-I. [1] |
激酶实验 | Migration assays: Assays are conducted in wells of a 24-well, 8 μm pore size Transwell plate. A 6.5-mm insert membrane is coated with 0.1 mL COL-I (300 μg/mL in MEGM) and then air dried for 16 hours. The collagen coating is rehydrated for 1 hour in 0.2 mL MEGM. The inner chamber contains MEGM-10% FBS as a chemoattractant. The compounds (10–100 μmol/L) or DMSO (0.1%–1%) are added to both inner and outer chambers. Before plating in the outer chamber, cells (5×104) are coincubated for 20 minutes with the compounds or DMSO in MEGM. Cells are allowed to migrate for 16 to 18 hours. The cells remaining on the top surface of the membrane are removed with a cotton swab. The cells on the bottom surface of the membrane are fixed and stained (0.2% crystal violet). The incorporated dye is extracted with 1% SDS and the A570 is measured. |
细胞实验 | Assays are conducted in wells of a 96-well flat bottom, white wall plates. 184B5-MT and MCF7-β3/MT cells (5×104) are grown for 16 hours in MEGM-10% FBS and DMEM-10% FBS, respectively. 184B5-MT cells are replenished with fresh MEGM (0.1 mL per well) and incubated for an additional 24 hours in the presence of the compounds (100 μM) or vehicle (1% DMSO). MCF7-β3/MT cells are replenished with fresh DMEM-10% FBS (0.1 mL per well) and incubated for an additional 6 hours in the presence of the compounds (400 μM) or vehicle (2% DMSO). The viable cells are counted using a luminescent ATP-Lite assay.(Only for Reference) |
分子量 | 260.16 |
分子式 | C12H15Cl2NO |
CAS No. | 7497-07-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 26 mg/mL (100 mM)
Ethanol: 26 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.8438 mL | 19.2189 mL | 38.4379 mL | 96.0947 mL |
5 mM | 0.7688 mL | 3.8438 mL | 7.6876 mL | 19.2189 mL | |
10 mM | 0.3844 mL | 1.9219 mL | 3.8438 mL | 9.6095 mL | |
20 mM | 0.1922 mL | 0.9609 mL | 1.9219 mL | 4.8047 mL | |
50 mM | 0.0769 mL | 0.3844 mL | 0.7688 mL | 1.9219 mL | |
100 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9609 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。
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