2. Metabolic Enzyme/Protease
  3. MMP
  4. Marimastat

Marimastat  (Synonyms: BB2516; TA2516)

Cat. No.: HY-12169 Purity: 99.81%
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Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.

For research use only. We do not sell to patients.

Marimastat Chemical Structure

Marimastat Chemical Structure

CAS No. : 154039-60-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 68 In-stock
5 mg USD 106 In-stock
10 mg USD 158 In-stock
50 mg USD 462 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Marimastat Related Antibodies

Top Publications Citing Use of Products

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes[1][2].

IC50 & Target[1]

MMP-3

3 nM (IC50)

MMP-1

5 nM (IC50)

MMP-2

6 nM (IC50)

MMP-14

9 nM (IC50)

MMP-7

13 nM (IC50)

In Vitro

Marimastat (BB2516) (1 μM) shows inhibition of vascular outgrowth, and selectively affects angiogenesis[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Marimastat Related Antibodies
In Vivo

Animals receiving chemoradiation + Marimastat (BB2516) (8.7 mg/kg) have statistically significant delayed growth, compared to animals receiving chemoradiation alone. Marimastat (BB2516) may work in combination with chemotherapy and radiation to inhibit tumor growth[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

331.41

Formula

C15H29N3O5
CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=C(NO)[C@@H](O)[C@@H](CC(C)C)C(N[C@H](C(NC)=O)C(C)(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (301.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0174 mL 15.0871 mL 30.1741 mL
5 mM 0.6035 mL 3.0174 mL 6.0348 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

Compounds 1, 2, 7-9 and 11-16 are pre-incubated with MMP-1 or MMP-3 (10 nM) at different concentrations (0-10 μM) in a mixture of Tris-HCl (50 mM, pH 7.5), NaCl (150 mM), CaCl2 (10 mM), NaN3 (0.02%) and Brij-35 (0.05%) for 1 hour at 37°C. Residual activity is measured using the fluorogenic MMP substrate (2 μM) by fluorescence increase (emission at 393 nm and excitation at 325 nm) on a fluorescence plate reader. The data are fitted to the tight binding inhibitor equation: v=[(E-I-k+[(E-I-k)2+4Ek]1/2)/(2E)], where v is the velocity of the reaction, E is the enzyme concentration, I is the initial inhibitor concentration, and k is the apparent inhibition constant, using the software Prism.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Three-month-old female nude mice are inoculated using a trochar needle with 2 mm2 established SCC-1 tissue subcutaneously in the flank. Treatment started once the tumors are 5-6 mm in diameter. Mice are randomLy divided into groups of 8 mice to receive different treatments: (1) control, (2) marimastat alone, (3) cisplatin + radiation in combination and (4) marimastat + cisplatin + radiation in combination. All animalsreceive a 14-day osmotic pump containing dimethylsulfoxide (DMSO) as a control for both the pump and vehicle. Animals treated with marimastatreceive the same osmotic pump containing 200 μL of marimastat with DMSO to result in a daily dose of 8.7 mg/kg 10 days after the initiation of treatment. Lead-shielded animalsreceive 8 Gy of 60Co radiation to the exposed tumor, divided into 4 fractions on days 8, 12, 16 and 20. A dose of 8 Gy is chosen because 7.5 Gy (7,500 rad) has been shown in previous experiments to inhibit tumor growth without being a curative dose. Animals receive 4 intraperitoneal doses of cisplatin (3 mg/kg) 1 h before each fraction of radiation. Tumors are measured biweekly for 32 days. Potential treatment toxicity is monitored using mouse weight. Tumor size (surface area equal to product of two largest diameters) and regression rates are determined in each treatment group. After 32 days, tumors are harvested for immunohistochemistry. Day 32 is chosen due to death of control group animals and euthanization of animals showing clinical signs of illness to allow for statistical analysis of data acquired from surviving animals.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0174 mL 15.0871 mL 30.1741 mL 75.4353 mL
5 mM 0.6035 mL 3.0174 mL 6.0348 mL 15.0871 mL
10 mM 0.3017 mL 1.5087 mL 3.0174 mL 7.5435 mL
15 mM 0.2012 mL 1.0058 mL 2.0116 mL 5.0290 mL
20 mM 0.1509 mL 0.7544 mL 1.5087 mL 3.7718 mL
25 mM 0.1207 mL 0.6035 mL 1.2070 mL 3.0174 mL
30 mM 0.1006 mL 0.5029 mL 1.0058 mL 2.5145 mL
40 mM 0.0754 mL 0.3772 mL 0.7544 mL 1.8859 mL
50 mM 0.0603 mL 0.3017 mL 0.6035 mL 1.5087 mL
60 mM 0.0503 mL 0.2515 mL 0.5029 mL 1.2573 mL
80 mM 0.0377 mL 0.1886 mL 0.3772 mL 0.9429 mL
100 mM 0.0302 mL 0.1509 mL 0.3017 mL 0.7544 mL
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Marimastat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Marimastat154039-60-8BB2516 TA2516BB 2516BB-2516TA2516TA 2516TA-2516MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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