NSC 405020

製品コードS8072 バッチS807201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H15Cl2NO
分子量 260.16 CAS No. 7497-07-6
Solubility (25°C)* 体外 DMSO 52 mg/mL (199.87 mM)
Ethanol 52 mg/mL (199.87 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.
in vitro 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 (100μM) 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]
in vivo 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 184B5-MT and MCF7-β3/MT
濃度 ~400 μM
反応時間 24 or 30 h
実験の流れ 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.
動物実験 動物モデル BALB/c nu/nu mice injected with MCF7-β3/WT and MCF7-β3/ΔPEX cells
投薬量 0.5 mg/kg, 3 times per week
投与方法 Intratumoral injection

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

MMP14 expression and collagen remodelling support uterine leiomyosarcoma aggressiveness [ Mol Oncol, 2023, 10.1002/1878-0261.13440] PubMed: 37078535
Lymphocyte access to lymphoma is impaired by high endothelial venule regression [ Cell Rep, 2021, 37(4):109878] PubMed: 34706240
Protease Inhibitor-Dependent Inhibition of Light-Induced Stomatal Opening [ Front Plant Sci, 2021, 12:735328] PubMed: 34567048
Lymphatic endothelium stimulates melanoma metastasis and invasion via MMP14-dependent Notch3 and β1-integrin activation. [ Elife, 2018, 7] PubMed: 29712618
LIFR increases the release of soluble endoglin via the upregulation of MMP14 expression in preeclampsia. [ Reproduction, 2018, 155(3):297-306] PubMed: 29363569

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。