| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Ubenimex is a novel and potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor used in the treatment of acute myelocytic leukemia.
| ln Vitro |
In ATRA-sensitive APL NB4 cells, bestatin promotes ATRA-induced differentiation and prevents ATRA-driven p38 MAPK phosphorylation. ATRA-resistant APL MR2 cells' differentiation block was not reversed by bestatin. When CD13 binds to the anti-CD13 antibody WM-15, p38 MAPK is phosphorylated. This decreases Bestatin's suppression of p38 MAPK phosphorylation and totally removes Bestatin's stimulatory effect on ATRA-induced NB4 cell differentiation [2]. Cells treated with bestatin (600 μM) underwent slower cell cycle progression because their frequency of cell division and growth were decreased. Bestatin suppresses D's intrinsic multinucleation and mitotic frequency. discoideum and does not cause D cell death. discoideum cells at 0-600 μM doses. In PsaA-GFP and GFP-expressing cell lysates, bestatin reduced the aminopeptidase activity by 69.39% and 39.93% of the control, respectively [4].
|
|---|---|
| ln Vivo |
In diabetic mice, bestatin (20 μM) dramatically suppressed MMP-9-specific sol zone density and considerably decreased CD13 expression as compared to mice treated with diabetic vehicles. Diabetes-stricken mice's VEGF and heparanase expression were markedly suppressed by bestatin therapy. In the retina of diabetic mice, intravitreal betastatin therapy markedly reduced the production of VEGF and HIF-1α. Furthermore, the elevation of heparanase expression in diabetic mice's retina can be considerably suppressed by intravitreal betastatin injection [1]. When splenocytes are treated with Bestatin (10, 1, and 0.1 mg/kg, i.p.), they produce more hemolytic anti-SRBC antibodies (PFC) and more 2-ME-resistant serum before antigen-enhancing humoral responses to SRBC occur. Hemagglutinin titer (0.1 mg/kg) in dosage. Injecting mice with Bestin (1 and 0.1 mg/kg) five times every other day following cyclophosphamide injection did not alter the drug's inhibitory effect on the number of PFC and, in fact, produced a greater decrease in total anti-SRBC hemagglutinin at the antigen dosage. 1 mg/kg seven days following stimulation [3].
|
| References |
|
| Additional Infomation |
Ubenimex (also known as bestatin) is a competitive protease inhibitor. It is an inhibitor of aminopeptidase B, leukotriene A4 hydrolase, aminopeptidase N. It is being studied for use in the treatment of acute myelocytic leukemia.
Ubenimex has been reported in Streptomyces abikoensis and Streptomyces olivoreticuli with data available. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Ubenimex competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage and bone marrow stem cell as well as stimulates release of interleukin-1 and -2, thus further enhances its antitumor activity. Drug Indication An adjuvant therapy used for acute and chronic myelonous leukemia, lung cancer and nasopharyngeal cancer. It is also used to treat hypercholesterolaemia. |
| Molecular Formula |
C16H24N2O4
|
|---|---|
| Molecular Weight |
308.37
|
| Exact Mass |
308.173
|
| CAS # |
58970-76-6
|
| Related CAS # |
Bestatin hydrochloride;65391-42-6;Bestatin trifluoroacetate;223763-80-2
|
| PubChem CID |
72172
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
604.7±55.0 °C at 760 mmHg
|
| Melting Point |
245 °C (dec.)(lit.)
|
| Flash Point |
319.5±31.5 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.557
|
| LogP |
2.64
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
22
|
| Complexity |
367
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC(C)C[C@@H](C(=O)O)NC(=O)[C@H]([C@@H](CC1=CC=CC=C1)N)O
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~8.33 mg/mL (~27.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (2.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2429 mL | 16.2143 mL | 32.4286 mL | |
| 5 mM | 0.6486 mL | 3.2429 mL | 6.4857 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2429 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
