TMI-1
作者：齊岳
發(fā)布時(shí)間：2023-09-05
08:50:37
點(diǎn)擊數(shù)：
產(chǎn)品名稱：TMI-1
產(chǎn)品描述：
| 產(chǎn)品描述 | TMI-1, a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer. |
| 靶點(diǎn)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 |
| 體外活性 | 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] |
| 體內(nèi)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] |
| 別名 | WAY-171318 |
| 分子量 | 398.5 |
| 分子式 | C17H22N2O5S2 |
| CAS No. | 287403-39-8 |
存儲(chǔ)
| 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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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