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Batimastat sodium ( BB94 sodium), a synthetic hydroxamate analog and an anticancer drug developed by Laurie Hines of British Biotech, is a broad spectrum inhibitor of matrix metalloprotease (MMP) with potential antitumor activity. It inhibits MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively. It also inhibits the activitity of other metalloproteases, such as ADAM17. It exhibits antineoplastic and antiangiogenic activity in various tumor models, including ovarian carcinoma xegnografts and human colon tumor.
ln Vitro |
Batimastat (BB-94) is a strong inhibitor of matrix metalloproteinase that binds in an unusual way. Batimastat has an IC50 of 4 nM for gelatinases A and 10 nM for gelatinases B. Comparable to the results for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM)[2], the IC50 with the structurally identical collagenase Ht-d is 6 nM. This metalloproteinase inhibitor, Batimastat (BB-94, IC50=230 nM), is based on hydroxamic acid and successfully inhibits CD30 shedding from the cell line Karpas299[3].
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ln Vivo |
In an orthotopic model of human breast cancer, intrathecal treatment of Batimastat (BB-94) significantly inhibits the growth of human ovarian carcinoma xenografts and murine melanoma metastasis while delaying the growth of primary tumors without causing cytotoxicity or altering mRNA levels[2]. Antineoplastic and antiangiogenic properties have been demonstrated by the synthetic matrix metalloproteinase inhibitor batimastat (BB) -94 in a number of tumor types. All animals are alive and well on day 200 after receiving treatment with Batimastat (60 mg/kg ip every other day, for a total of eight injections) and Cisplatin (4 mg/kg iv, every seven days, for a total of three injections), which totally stops the growth and spread of both xenografts[4]. When compared to controls (75%), animals treated with Batimastat (BB-94) had higher survival rates (95.2%) according to Kaplan-Meier analysis of survival (at 48 hours), and these changes are nearly statistically significant (p=0.064)[5]. Four hours after E2 administration—the period at which collagen density is seen to be at its lowest following hormone treatment—matrix density is assessed in animals that have been pretreated with saline or Batimastat (40 mg/kg)[6].
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Animal Protocol |
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References |
[1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70.
[2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54. [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5. [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92. [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726. [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124 |
Molecular Formula |
C23H30N3O4S2-.NA+
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Molecular Weight |
499.6218
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CAS # |
130464-84-5
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Related CAS # |
Batimastat;130370-60-4
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SMILES |
[O-]NC([C@@H](CSC1=CC=CS1)[C@@H](CC(C)C)C(N[C@@H](CC2=CC=CC=C2)C(NC)=O)=O)=O.[Na+]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0015 mL | 10.0076 mL | 20.0152 mL | |
5 mM | 0.4003 mL | 2.0015 mL | 4.0030 mL | |
10 mM | 0.2002 mL | 1.0008 mL | 2.0015 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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