產(chǎn)品目錄

規(guī)格	1mg 5mg
CAS	287405-51-0
別名	TMI-005
化學名	(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
儲存條件	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

產(chǎn)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).

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術有限公司

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