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MedKoo Cat#: 406486 | Name: MPT0E028

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.)

Chemical Structure

MPT0E028
MPT0E028
CAS#1338320-94-7

Theoretical Analysis

MedKoo Cat#: 406486

Name: MPT0E028

CAS#: 1338320-94-7

Chemical Formula: C17H16N2O4S

Exact Mass: 344.0831

Molecular Weight: 344.38

Elemental Analysis: C, 59.29; H, 4.68; N, 8.13; O, 18.58; S, 9.31

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
MPT-0E028; MPT0E028; MPT 0E028; Imofinostatum; Imofinostat
IUPAC/Chemical Name
(E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide
InChi Key
MGTIFSBCGGAZDB-VQHVLOKHSA-N
InChi Code
InChI=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+
SMILES Code
O=C(NO)/C=C/C1=CC2=C(N(S(=O)(C3=CC=CC=C3)=O)CC2)C=C1
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
MPT0E028 enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells.        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6.
In vitro activity:
This study demonstrated that MPT0E028, a novel HDAC inhibitor, reduces the viability of B-cell lymphomas by inducing apoptosis and shows a more potent HDAC inhibitory effect compared to SAHA, the first HDAC inhibitor approved by the FDA. In addition to HDACs inhibition, MPT0E028 also possesses potent direct Akt targeting ability as measured by the kinome diversity screening assay. Also, MPT0E028 reduces Akt phosphorylation in B-cell lymphoma with an IC50 value lower than SAHA. Reference: Oncotarget. 2015 Mar 10;6(7):4976-91. https://pubmed.ncbi.nlm.nih.gov/25669976/
In vivo activity:
A mouse model of porcine pancreatic elastase (PPE)-induced emphysema was orally administered 0, 25, or 50 mg/kg body weight (BW) of the MPT0E028 five times/week for 3 weeks. 50 mg/kg BW of the MPT0E028 significantly decreased the tidal volume in emphysematous mice (p < 0.05). Emphysema severity was significantly reduced from 26.65% (PPE only) to 13.83% (50 mg/kg BW of the MPT0E028). Reference: Front Med (Lausanne). 2022 May 18;9:794025. https://pubmed.ncbi.nlm.nih.gov/35665319/
Solvent mg/mL mM comments
Solubility
DMSO 100.0 290.37
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 344.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Huang HL, Peng CY, Lai MJ, Chen CH, Lee HY, Wang JC, Liou JP, Pan SL, Teng CM. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6(7):4976-91. doi: 10.18632/oncotarget.3213. PMID: 25669976; PMCID: PMC4467128. 2. Huang HL, Lee HY, Tsai AC, Peng CY, Lai MJ, Wang JC, Pan SL, Teng CM, Liou JP. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. doi: 10.1371/journal.pone.0043645. Epub 2012 Aug 22. Erratum in: PLoS One. 2012;7(9). doi: 10.1371/annotation/ab4fff87-6a32-4718-aa4c-91658f164b8d. Huang, Han-Lin [corrected to Huang, Han-Li]. PMID: 22928010; PMCID: PMC3425516. 3. Yeh LY, Fang YT, Lee HS, Liu CH, Chen YY, Lo YC, Laiman V, Liou JP, Chung KF, Chuang HC, Lin CH. A Potent Histone Deacetylase Inhibitor MPT0E028 Mitigates Emphysema Severity via Components of the Hippo Signaling Pathway in an Emphysematous Mouse Model. Front Med (Lausanne). 2022 May 18;9:794025. doi: 10.3389/fmed.2022.794025. PMID: 35665319; PMCID: PMC9157428.
In vitro protocol:
1. Huang HL, Peng CY, Lai MJ, Chen CH, Lee HY, Wang JC, Liou JP, Pan SL, Teng CM. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6(7):4976-91. doi: 10.18632/oncotarget.3213. PMID: 25669976; PMCID: PMC4467128. 2. Huang HL, Lee HY, Tsai AC, Peng CY, Lai MJ, Wang JC, Pan SL, Teng CM, Liou JP. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. doi: 10.1371/journal.pone.0043645. Epub 2012 Aug 22. Erratum in: PLoS One. 2012;7(9). doi: 10.1371/annotation/ab4fff87-6a32-4718-aa4c-91658f164b8d. Huang, Han-Lin [corrected to Huang, Han-Li]. PMID: 22928010; PMCID: PMC3425516.
In vivo protocol:
1. Yeh LY, Fang YT, Lee HS, Liu CH, Chen YY, Lo YC, Laiman V, Liou JP, Chung KF, Chuang HC, Lin CH. A Potent Histone Deacetylase Inhibitor MPT0E028 Mitigates Emphysema Severity via Components of the Hippo Signaling Pathway in an Emphysematous Mouse Model. Front Med (Lausanne). 2022 May 18;9:794025. doi: 10.3389/fmed.2022.794025. PMID: 35665319; PMCID: PMC9157428. 2. Huang HL, Lee HY, Tsai AC, Peng CY, Lai MJ, Wang JC, Pan SL, Teng CM, Liou JP. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. doi: 10.1371/journal.pone.0043645. Epub 2012 Aug 22. Erratum in: PLoS One. 2012;7(9). doi: 10.1371/annotation/ab4fff87-6a32-4718-aa4c-91658f164b8d. Huang, Han-Lin [corrected to Huang, Han-Li]. PMID: 22928010; PMCID: PMC3425516.
1: Chen CH, Chen MC, Wang JC, Tsai AC, Chen CS, Liou JP, Pan SL, Teng CM. Synergistic Interaction between the HDAC Inhibitor, MPT0E028, and Sorafenib in Liver Cancer Cells In Vitro and In Vivo. Clin Cancer Res. 2014 Mar 1;20(5):1274-87. doi: 10.1158/1078-0432.CCR-12-3909. Epub 2014 Feb 11. PubMed PMID: 24520095. 2: Chen MC, Chen CH, Wang JC, Tsai AC, Liou JP, Pan SL, Teng CM. The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells. Cell Death Dis. 2013 Sep 19;4:e810. doi: 10.1038/cddis.2013.330. PubMed PMID: 24052078; PubMed Central PMCID: PMC3789188. 3: Huang HL, Lee HY, Tsai AC, Peng CY, Lai MJ, Wang JC, Pan SL, Teng CM, Liou JP. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. doi: 10.1371/journal.pone.0043645. Epub 2012 Aug 22. Erratum in: PLoS One. 2012;7(9). doi: 10.1371/annotation/ab4fff87-6a32-4718-aa4c-91658f164b8d. Huang, Han-Lin [corrected to Huang, Han-Li]. PubMed PMID: 22928010; PubMed Central PMCID: PMC3425516.