MPT0E028

CAS 1338320-94-7 MFCD438320947

化学结构图

1338320-94-7
SMILES: O=C(/C=C/c1ccc2c(c1)CCN2S(=O)(=O)c1ccccc1)NO

化学属性

Mol. Weight344.38494
Appearance white solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Chemical NameMPT0E028
FormulaC17H16N2O4S
Synonym MPT-0E028; MPT0E028; MPT 0E028
IUPAC Name(E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide
InChIKeyMGTIFSBCGGAZDB-VQHVLOKHSA-N
InChIInChI=1S/C17H16N2O4S/c20-17(18-21)9-7-13-6-8-16-14(12-13)10-11-19(16)24(22,23)15-4-2-1-3-5-15/h1-9,12,21H,10-11H2,(H,18,20)/b9-7+
Canonical SMILESO=C(NO)/C=C/C1=CC2=C(N(S(=O)(C3=CC=CC=C3)=O)CC2)C=C1
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产品应用

  • MPT0E028 is a novel N-hydroxyacrylamide-derived HDAC inhibitor, inhibited human colorectal cancer HCT116 cell growth in vitro and in vivo. The results of NCI-60 screening showed that MPT0E028 inhibited proliferation in both solid and hematological tumor cell lines at micromolar concentrations, and was especially potent in HCT116 cells. MPT0E028 had a stronger apoptotic activity and inhibited HDACs activity more potently than SAHA, the first therapeutic HDAC inhibitor proved by FDA. In vivo murine model, the growth of HCT116 tumor xenograft was delayed and inhibited after treatment with MPT0E028 in a dose-dependent manner. Based on in vivo study, MPT0E028 showed stronger anti-cancer efficacy than SAHA. No significant body weight difference or other adverse effects were observed in both MPT0E028-and SAHA-treated groups. Taken together, our results demonstrate that MPT0E028 has several properties and is potential as a promising anti-cancer therapeutic drug. ( PLoS One. 2012;7(8):e43645.)

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类

  1. Medical Research Areas
  2. Neuronal Signaling
  3. HDAC

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