| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Acivicin (AT-125) is a novel, potent and naturally occurring inhibitor of gamma-glutamyl transferase (GGT) with anti-cancer and anti-parasitic activity. It is a natural product isolated from Streptomyces sviceus.
| ln Vitro |
In human HepG2 cells, acivicin (AT-125; 0.1-50 μM; 5 days) possesses an IC50 of 0.7 μM [1].
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|---|---|
| ln Vivo |
Urinary γ-GT can be reduced by 70–778% with Acivicin (AT-125; 5 mg/kg; intraperitoneal injection; twice weekly) [3].
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| Animal Protocol |
Animal/Disease Models: Male pigmented Long-Evans rats, weighing between 250 g and 300 g, exposed to toluene [3]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; twice weekly (Monday and Wednesday) Experimental Results: Urinary γ-GT diminished by 70-78%. |
| References |
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| Additional Infomation |
Acivicin is an L-alpha-amino acid that is L-alanine in which the methyl group is replaced by a (5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl group. A glutamine analogue antimetabolite, it interferes with glutamate metabolism and several glutamate-dependent synthetic enzymes. It is obtained as a fermentation product of Streptomyces sviceus bacteria. It has a role as an antimetabolite, a metabolite, an antineoplastic agent, an EC 2.3.2.2 (gamma-glutamyltransferase) inhibitor, an antimicrobial agent, an antileishmanial agent and a glutamine antagonist. It is a member of isoxazoles, an organochlorine compound and a non-proteinogenic L-alpha-amino acid.
Acivicin is a modified amino acid and structural analog of glutamine. Acivicin inhibits glutamine amidotransferases in the purine and pyrimidine biosynthetic pathways, thereby inhibiting tumor growth in cell lines dependent on glutamine metabolism. (NCI04) |
| Molecular Formula |
C5H7CLN2O3
|
|---|---|
| Molecular Weight |
178.57368
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| Exact Mass |
178.014
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| CAS # |
42228-92-2
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| Related CAS # |
Acivicin hydrochloride;161922-40-3
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| PubChem CID |
294641
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| Appearance |
White to light yellow solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
341.6±48.0 °C at 760 mmHg
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| Melting Point |
>200ºC (dec.)
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| Flash Point |
160.4±29.6 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.664
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| LogP |
-0.31
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
11
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| Complexity |
206
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H](ON=C1Cl)[C@@H](C(=O)O)N
|
| InChi Key |
QAWIHIJWNYOLBE-OKKQSCSOSA-N
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| InChi Code |
InChI=1S/C5H7ClN2O3/c6-3-1-2(11-8-3)4(7)5(9)10/h2,4H,1,7H2,(H,9,10)/t2-,4-/m0/s1
|
| Chemical Name |
(2S)-Amino[(5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl]ethanoic acid
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| Synonyms |
Acivicin AT125U 42126NSC-163501AT-125U-42126NSC 163501 Antibiotic AT-125
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| HS Tariff Code |
2934.99.9001
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| 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 (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
H2O : ~6.67 mg/mL (~37.35 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.6000 mL | 28.0002 mL | 56.0004 mL | |
| 5 mM | 1.1200 mL | 5.6000 mL | 11.2001 mL | |
| 10 mM | 0.5600 mL | 2.8000 mL | 5.6000 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02989571 | Completed | Drug: Intravenous normal saline administered at 125ml/hr |
Labor; Forced or Induced, Affecting Fetus or Newborn |
MemorialCare Health System | March 2016 | Early Phase 1 |
| NCT02966379 | Completed | Device: cochlear implantation | Cochlear Implant | Oticon Medical | March 30, 2016 | Not Applicable |
| NCT01973725 | Completed | Drug: Icotinib Hydrochloride | Esophageal Squamous Cell Carcinoma | Yuhong Li | October 2013 | Phase 2 |
| NCT00580827 | Completed | Drug: Placebo Drug: Disulfiram |
Cocaine-Related Disorder Opiate Dependence |
Yale University | September 2003 | Not Applicable |
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