| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Batimastat (formerly known as BB-94), 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. With an IC50 of 3 nM, 4 nM, 4 nM, 6 nM, and 20 nM, respectively, it inhibits MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3. Moreover, it suppresses the activity of other metalloproteases, including ADAM17. In a number of tumor models, such as human colon tumors and ovarian carcinoma xegnografts, it demonstrates antiangiogenic and antineoplastic properties.
| Targets |
MMP-1 (IC50 = 3 nM); MMP-2 (IC50 = 4 nM); MMP-9 (IC50 = 4 nM); MMP-7 (IC50 = 6 nM); MMP-7 (IC50 = 6 nM)
|
|---|---|
| ln Vitro |
Batimastat (BB-94) is a potent, broad-spectrum matrix metalloprotease (MMP) inhibitor with IC50 values of 3 nM, 4 nM, 4 nM, 6 nM, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3, respectively.[1]
Batimastat has a thiophene ring that is deeply inserted into the primary specificity site, displaying an unexpected binding geometry.[2] |
| ln Vivo |
Batimastat has the ability to stop the growth and metastasis of B16-BL6 murine melanoma.[1]
Timastat treatment inhibits the growth of the primary tumor by 50%, the spread of the tumor locally and regionally by 35%, and the spread of the tumor distantly by 10% in an orthotopic colon tumor model in mice.[3] Batimastat inhibits the in vivo growth of experimental hemangiomas, most likely through preventing the transformed cells from recruiting endothelial cells or by disrupting the arrangement of cells in vascular structures.[4] |
| Enzyme Assay |
In vitro, batimastat IC50s are calculated using enzyme assays against various metalloproteinases.
|
| Cell Assay |
The IC50 was determined after incubating the cells for 22 hours at various concentrations of batimastat that had been dissolved in absolute ethanol.
|
| Animal Protocol |
Mice: Female BALB/c mice six weeks of age are employed. One hour prior to and twenty-four hours following infection, mice receive intraperitoneal injections of Batimastat (BB-94, 50 mg/kg). 50 mg/mL of batimastat is suspended in DMSO and kept frozen at -20°C. It is diluted 20 times in phosphate buffered saline (PBS) before use, and 500 μL is injected into the animals. A 500 μL injection of 5% DMSO in PBS is given to control mice. 48 hours after the ic challenge, animals are sacrificed.
Rats: Sprague-Dawley female rats receive an intraperitoneal (i.p.) injection of a single physiological dose of E2 (40 μg/kg in a 0.9% NaCl, 0.4% EtOH vehicle) at predetermined intervals before tissue is collected during necropsy. It has been demonstrated that the uterine wet weight, tissue architecture, and gene expression changes that are indicative of estrogen receptor activation are brought about by this in vivo dose level of estrogen. In each study, the animals are given a single 40 μg/kg bolus of E2 intraperitoneally four hours before tissue collection, and the control group is given only a vehicle. In vivo MMP inhibition has been demonstrated by batimastat when given intraperitoneally (i.p.) at a dose of 40 mg/kg in a 1× PBS, 0.1% Tween-20 vehicle, 4 hours before E2 or saline control. |
| References |
| Molecular Formula |
C23H31N3O4S2
|
|---|---|
| Molecular Weight |
477.64
|
| Exact Mass |
477.18
|
| Elemental Analysis |
C, 57.84; H, 6.54; N, 8.80; O, 13.40; S, 13.43
|
| CAS # |
130370-60-4
|
| Related CAS # |
Batimastat sodium salt;130464-84-5
|
| Appearance |
white solid powder
|
| SMILES |
CC(C)C[C@H]([C@H](CSC1=CC=CS1)C(=O)NO)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)NC
|
| InChi Key |
XFILPEOLDIKJHX-QYZOEREBSA-N
|
| InChi Code |
InChI=1S/C23H31N3O4S2/c1-15(2)12-17(18(22(28)26-30)14-32-20-10-7-11-31-20)21(27)25-19(23(29)24-3)13-16-8-5-4-6-9-16/h4-11,15,17-19,30H,12-14H2,1-3H3,(H,24,29)(H,25,27)(H,26,28)/t17-,18+,19+/m1/s1
|
| Chemical Name |
(2S,3R)-N-hydroxy-N'-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide
|
| Synonyms |
Batimastat; BB94; BB-94; BB 94
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0936 mL | 10.4681 mL | 20.9363 mL | |
| 5 mM | 0.4187 mL | 2.0936 mL | 4.1873 mL | |
| 10 mM | 0.2094 mL | 1.0468 mL | 2.0936 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.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
