产品属性：
产品名称 | 规格 | CAS号 | 型号 |
Apratastat | 1mg 5mg | 287405-51-0 | EY-Y0163844 |
Cas No.287405-51-0
别名 TMI-005
化学名 (3S)-N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide
分子式 C17H22N2O6S2
分子量 414.5
溶解度 10mg/mL in ethanol, 25mg/mL in DMSO, or in DMF
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
TMI-005 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE), matrix metalloproteinase-1 (MMP-1), and MMP-13 (IC50s = 20, 33, and 8.1 nM, respectively).[1] It inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml).[2] TMI-005 (25 μM) reduces basal and ionizing radiation-induced secretion of the ADAM17/TACE substrates ALCAM and amphiregulin from A549 and NCI H125 cells.[3]It inhibits proliferation of A549 cells when used at concentrations of 25 and 50 μM and sensitizes A549 and NCI H125 cells to ionizing radiation at 25 μM. TMI-005 (25 mg/kg twice per day) reduces tumor growth in an A549 mouse xenograft model when administered in combination with ionizing radiation.
Reference:
[1]. Levin, J.I., Chen, J.M., and Cole, D.C. Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors. WO 00/44709, (2000).
[2]. Shu, C., Zhou, H., Afsharvand, M., et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: A population-based approach. J. Clin. Pharmacol. 51(4), 472-481 (2011).
[3]. Sharma, A., Bender, S., Zimmerman, M., et al. Secretome signature identifies ADAM17 as novel target for radiosensitization of non-small cell lung cancer. Clin. Cancer Res. 22(17), 4428-4439 (2016).
关键字： 287405-51-0;C17H22N2O6S2;Apratastat;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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