TMI-1
作者：齐岳
发布时间：2023-09-05
08:50:37
点击数：
产品名称：TMI-1
产品描述：
| 产品描述 | TMI-1, a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer. |
| 靶点活性 | ADAM10:16 nM(ki), MMP-9:12 nM, MMP-13:3 nM, ADAM17/TACE inhibitor:8.4 nM (IC50), MMP-14:26 nM, ADAM17/TACE:0.079 nM(ki), TNF-α secretion(THP-1 cells):200 nM, ADAM-TS-4:100 nM, MMP-2:4.7 nM, ADAM12:1.8 nM(ki), ADAM8:21 nM(ki), MMP-7:26 nM, TNF-α secretion(Raw cell):40 nM, MMP-1:6.6 nM |
| 体外活性 | TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC50s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC50s = 190 and 300 nM, respectively).[1]It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC50 values of less than 100 nM without inhibiting TNF-α expression in vitro.[3] |
| 体内活性 | TMI 1 inhibits LPS-induced TNF-α production in mice (ED50 = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED50s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.[3] |
| 别名 | WAY-171318 |
| 分子量 | 398.5 |
| 分子式 | C17H22N2O5S2 |
| CAS No. | 287403-39-8 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 35.9 mg/mL (410.4 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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