Marimastat(BB2516)CAS号: 154039-60-8分子式: C15H29N3O5分子量: 331.41描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
描述 |
Marimastat (BB-2516)是一种广谱的 matrix metalloprotease (MMP) 抑制剂,对 MMP-9,MMP-1,MMP-2,MMP-14 和 MMP-7 的 IC50 分别为 3 nM,5 nM,6 nM,9 nM 和 13 nM。 |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
马立马司他;BB2516;BB-2516;TA2516
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外观 |
白色粉末
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可溶性/溶解性 |
DMSO : 33.1 mg/mL (100 mM)
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生物活性 | |
靶点 |
MMP-9 ,MMP-1 ,MMP-2 ,MMP-14 ,MMP-7
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In vitro(体外研究) |
Marimastat (100 nM) significantly inhibits the expression of MMP14 in U251, U87, GBM39, and GBM43 tumor cells. Marimastat specifically inhibits the growth of glioma cells and has no effect on normal human astrocytes (NHA). Marimastat early down-regulates the expression of Notch target genes, such as Hes1 and Hes5.
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In vivo(体内研究) |
In an orthotopic oral squamous cell carcinoma implantation model, marimastat (150 mg/kg/day, p.o.) administered by an osmotic pump significantly suppresses the cervical lymph node metastasis and activation of MMP-2, and has a significantly better survival than control group. Marimastat reduces MMP hyperactivity of polycystic human and rat cholangiocytes and blocks the cystic expansion of PCK cholangiocytes. Chronic treatment of 8-week-old PCK rats with marimastat inhibits hepatic cystogenesis and fibrosis.
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参考文献 | |
参考文献 |
[1] Rasmussen HS, et al. Pharmacol Ther. 1997, 75(1), 69-75. [2] auf dem Keller U, et al. Cancer Res. 2010, 70(19), 7562-7569. [3] Ulasov I, et al. Cancer Med.?013, 2(4), 457-467. [4] Sinno M, et al. Stem Cells Dev. 2013, 22(3), 345-358. [5] Maekawa K, et al. Clin Exp Metastasis. 2002, 19(6), 513-518. [6] Urribarri AD, et al. Gut. 2014, 63(10), 1658-1667. |
分子结构图