Marimastat (BB-2516)

Catalog No.S7156

Marimastat (BB-2516) Chemical Structure

Molecular Weight(MW): 331.41

Marimastat (BB-2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.

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Biological Activity

Description Marimastat (BB-2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.
Targets
MMP-9 [1]
(cell-free assay)
MMP-1 [1]
(cell-free assay)
MMP-2 [1]
(cell-free assay)
MMP-14 [1]
(cell-free assay)
MMP-7 [1]
(cell-free assay)
3 nM 5 nM 6 nM 9 nM 16 nM
In vitro

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).[3] Marimastat early down-regulates the expression of Notch target genes, such as Hes1 and Hes5.[4]

In vivo 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.[5] 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.[6]

Protocol

Kinase Assay:[2]
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Inhibitor kinetics:

Recombinant human MMP2 is activated with 1 mM of 4-aminophenylmercuric acetate for 1 hour at 37°C. Rates of cleavage of 1 μM of the quenched fluorescent MMP substrate (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-[3-(2,4-dinitrophenyl)-L-2,3-diaminoproprionyl]-Ala-Arg-NH2 are measured in 96-well fluorimetry plates at 37°C 100 mM Tris-HCl (pH 7.5), 100 mM NaCl, 10 mM CaCl2, 0.05% Brij 35 using a 320 nm excitation filter and a 405 nm emission filter in the presence of increasing inhibitor concentrations. Curve-fitting and IC50 calculations are done using GraphPad Prism 5.0 Software.
Animal Research:[5]
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  • Animal Models: Orthotopic oral squamous cell carcinoma implantation model
  • Formulation: 50% DMSO (v/v) in PBS.
  • Dosages: 150 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (162.94 mM)
Ethanol 7 mg/mL warmed (21.12 mM)
Water Insoluble
In vivo Add solvents individually and in order:
50% DMSO+PBS
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 331.41
Formula

C15H29N3O5

CAS No. 154039-60-8
Storage powder
Synonyms

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00261391 Completed Vascular Anomalies Boston Children’s Hospital October 2000 Phase 1
NCT00003010 Completed Breast Cancer Eastern Cooperative Oncology Group|National Cancer Institute (NCI)|North Central Cancer Treatment Group September 1997 Phase 3
NCT00003011 Completed Lung Cancer NCIC Clinical Trials Group|Canadian Cancer Trials Group March 1997 Phase 3
NCT00002911 Completed Lung Cancer ILEX Oncology Services, Incorporated|National Cancer Institute (NCI) December 1996 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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MMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID