|Apratastat 目录号 GC35377|
Sample solution is provided at 25 µL, 10mM.
|Cas No.||287405-51-0||SDF||Download SDF|
|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
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). It inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml). 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.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.
. Levin, J.I., Chen, J.M., and Cole, D.C. Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors. WO 00/44709, (2000).
. 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).
. 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).