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Purity: =98.22%
Streptozotocin (also known as NSC-85998, STZ, Streptozotocin; U 9889) is a glucosamine-nitrosourea derivative and a potent DNA-methylating agent with IC50s of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells respectively. Streptozotocin is an antibiotic, methylating, carcinogen, and inducer of diabetes. Antineoplastic antibiotic streptozocin is methylnitrosourea that was extracted from the Streptomyces achromogenes bacteria. DNA is alkylated by streptozocin, which also prevents DNA synthesis and creates interstrand cross-links. This agent is easily absorbed by pancreatic beta cells because of its glucose moiety, which causes diabetes mellitus at high concentrations.
Targets |
DNA alkylator
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Streptozocin is an effective agent that methylates DNA; in HL60, K562, and C1498 cells, it has IC50 values of 11.7, 904, and 1024 μg/mL, respectively.
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Cell Assay |
In 96-well plates, human and murine cell lines are cultivated in triplicate at a density of 2×104 cells/well, either in the absence (untreated control) or in the presence of different concentrations of ALX (20-3000 μg/mL) or STZ (1-3000 μg/mL) for 48 hours at 37°C in a humidified atmosphere with 5% CO2. The experiments used cells cultured in complete medium as a control, and cells cultured in dH2O at a final concentration of 0.1% as a control for solvent toxicity. The MTT assay is used in accordance with the manufacturer's instructions to determine the effects of the tested drugs on the growth or viability of tumor cells. GraphPad Prism 4 is used to calculate the IC50 values, or drug concentrations that cause a 50% inhibition of cell growth.
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Animal Protocol |
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References |
Molecular Formula |
C8H15N3O7
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Molecular Weight |
265.22
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Exact Mass |
265.09
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Elemental Analysis |
C, 36.23; H, 5.70; N, 15.84; O, 42.23
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CAS # |
18883-66-4
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Appearance |
Solid powder
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SMILES |
CN(C(=O)N[C@@H]1[C@H]([C@@H]([C@H](O[C@@H]1O)CO)O)O)N=O
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InChi Key |
ZSJLQEPLLKMAKR-GKHCUFPYSA-N
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InChi Code |
InChI=1S/C8H15N3O7/c1-11(10-17)8(16)9-4-6(14)5(13)3(2-12)18-7(4)15/h3-7,12-15H,2H2,1H3,(H,9,16)/t3-,4-,5-,6-,7+/m1/s1
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Chemical Name |
1-methyl-1-nitroso-3-[(2S,3R,4R,5S,6R)-2,4,5-trihydroxy-6-(hydroxymethyl)oxan-3-yl]urea
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.84 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (7.84 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 20.8 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: ≥ 2.08 mg/mL (7.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 100 mg/mL (377.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.7705 mL | 18.8523 mL | 37.7045 mL | |
5 mM | 0.7541 mL | 3.7705 mL | 7.5409 mL | |
10 mM | 0.3770 mL | 1.8852 mL | 3.7705 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 |
NCT03351296 | Recruiting | Drug: Streptozocin Drug: Capecitabine |
Pancreatic Cancer | Gustave Roussy, Cancer Campus, Grand Paris |
June 26, 2018 | Phase 2 |
NCT00448136 | Completed | Drug: Streptozotocin Drug: 5 FU |
Neoplasms | Hoffmann-La Roche | July 2007 | Phase 2 |
NCT00004688 | Completed | Drug: streptozocin Drug: mercaptopurine |
Mixed Gliomas Anaplastic Astrocytoma |
Emory University | August 1996 | Phase 2 |
NCT00602082 | Completed | Drug: cisplatin Drug: streptozocin |
Gastrointestinal Carcinoid Tumor Islet Cell Tumor |
Cambridge University Hospitals NHS Foundation Trust |
August 2005 | Phase 2 |
Blood glucose values (top row) and body weight (bottom row) in response to insulin (glargine) treatment (U/kg daily) after diabetes induction by using STZ in male nude mice from Charles River Laboratories (CRL), Jackson Laboratories (JAX), and Taconic Farms (TAC). Comp Med . 2011 Aug;61(4):356-60. td> |