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Streptozocin

Catalog No.GC17131

Streptozocin Chemical Structure

Streptozocin, a potent DNA-methylating antibiotic, is a naturally occurring nitrosoamide used for extensively to produce diabetes in experimental models.

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10mM (in 1mL DMSO)
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100mg
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500mg
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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Protocol

Cell experiment [1]:

Cell lines

islet cells

Preparation Method

Monolayer cultures of islet cells from neonatal rats were exposed to concentrations of MNU and STZ (Streptozocin) of 1, 2, 5, or 10 mM, and the activity of the enzyme was assayed.

Reaction Conditions

1, 2, 5, or 10 mM

Applications

Streptozocin is toxic to cultured p-cells at a concentration of 1 mM.

Animal experiment [2]:

Animal models

Female mice

Preparation Method

Female mice received a single subdiabetogenic dose of streptozocin (65 mg/kg intraperitoneally) 8-11 days or 14-17 days before fertilization.

Dosage form

65 mg/kg; i.p.

Applications

Morphological analysis of preimplantation embryos collected on day 3 of pregnancy revealed significant changes in the distribution pattern of preimplantation embryo stages recovered from streptozocin-treated females.

References:

[1]. Wilson GL, et al. Mechanisms of nitrosourea-induced beta-cell damage. Activation of poly (ADP-ribose) synthetase and cellular distribution. Diabetes. 1988 Feb;37(2):213-6.

[2]. Veselá J, et al. Subdiabetogenic streptozocin treatment impairs preimplantation development of mouse embryos. Physiol Res. 1993;42(1):23-7.

Background

Streptozocin, a potent DNA-methylating antibiotic, is a naturally occurring nitrosoamide used for extensively to produce diabetes in experimental models.[1]

In vitro, STZ was toxic with IC50 values of 11.7, 904 and 1024 μg/ml for HL60, K562 and C1498 cells respectively.[3]

In vivo efficacy test it shown that when combined with a protocol for induction of diuresis, dogs were treated safely with 500 mg/m2 of streptozocin, intravenously, every 3 weeks, and it may be have a potential efficacy on the treatment of dogs with metastatic pancreatic islet cell tumors.[1]

In vivo experiment it indicated that mice were administrated streptozocin with 65 mg/kg intraperitoneally for 8-11 days or 14-17 days, streptozocin improved the impaired development of preimplantation embryos on 8-11 days. However, after 14-17 days, the incidence of degenerated embryos was increased in both streptozocin-treated mice groups.[2] Treatment with 60 mg/kg of streptozocin intravenously also induces an early hyperglycaemia when the hepatic glycogen storage is almost depleted that is during the fasting state.[4] For the treatment of advanced islet-cell carcinoma, the combination of streptozocin and doxorubicin is more efficious than the current standard regimen of streptozocin plus fluorouracil.[5] There is little value for patients with malignant carcinoid tumors by combination treatment with streptozocin and 5-fluorouracil.[6]

References:
[1].Moore AS, et al. Streptozocin for treatment of pancreatic islet cell tumors in dogs: 17 cases (1989-1999). J Am Vet Med Assoc. 2002 Sep 15;221(6):811-8.
[2].Veselá J, et al. Subdiabetogenic streptozocin treatment impairs preimplantation development of mouse embryos. Physiol Res. 1993;42(1):23-7.
[3].Diab RA, et al. Immunotoxicological effects of streptozotocin and alloxan: in vitro and in vivo studies. Immunol Lett. 2015 Feb;163(2):193-8.
[4].Wong KK. Reduction by streptozocin of blood glucose utilization during the appearance of the streptozocin induced early hyperglycaemia in fasting rats. Biochem Mol Biol Int. 1996 May;39(1):191-5.
[5].Moertel CG, et al. Streptozocin-doxorubicin, streptozocin-fluorouracil or chlorozotocin in the treatment of advanced islet-cell carcinoma. N Engl J Med. 1992 Feb 20;326(8):519-23.
[6].Oberg K, et al. Cytotoxic treatment in patients with malignant carcinoid tumors. Response to streptozocin--alone or in combination with 5-FU. Acta Oncol. 1987;26(6):429-32.

Chemical Properties

Cas No. 18883-66-4 SDF
Synonyms Streptozotocin; U 9889; STZ
Chemical Name 1-methyl-1-nitroso-3-[2,4,5-trihydroxy-6-(hydroxymethyl)oxan-3-yl]urea
Canonical SMILES CN(C(=O)NC1C(C(C(OC1O)CO)O)O)N=O
Formula C8H15N3O7 M.Wt 265.22
Solubility ≥ 10.3mg/mL in DMSO, ≥ 53.2mg/mL in H2O, ≥ 26.5mg/mL in EtOH with gentle warming Storage 4°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Research Update

Streptozocin (Zanosar)

Med Lett Drugs Ther1982 Nov 12;24(622):100-1.PMID: 6290862DOI: 10.1002/0471141755.ph0547s40

Streptozotocin (STZ) is an antibiotic that can cause pancreatic β-cell destruction, so it is widely used experimentally as an agent capable of inducing insulin-dependent diabetes mellitus (IDDM), also known as type 1 diabetes mellitus (T1DM). This unit describes protocols for the production of insulin deficiency and hyperglycemia in mice and rats, using STZ. These models for diabetes can be employed for assessing the mechanisms of T1DM, screening potential therapies for the treatment of this condition, and evaluation of therapeutic options.

Streptozotocin-induced diabetic models in mice and rats

Curr Protoc Pharmacol2008 Mar;Chapter 5:Unit 5.47.PMID: 22294227DOI: 10.1002/0471141755.ph0547s40

Streptozotocin (STZ) is an antibiotic that can cause pancreatic β-cell destruction, so it is widely used experimentally as an agent capable of inducing insulin-dependent diabetes mellitus (IDDM), also known as type 1 diabetes mellitus (T1DM). This unit describes protocols for the production of insulin deficiency and hyperglycemia in mice and rats, using STZ. These models for diabetes can be employed for assessing the mechanisms of T1DM, screening potential therapies for the treatment of this condition, and evaluation of therapeutic options.

Streptozocin: a review of its pharmacology, efficacy, and toxicity

Cancer Treat Rep1982 Mar;66(3):427-38.PMID: 6277485DOI: 10.1016/j.ijbiomac.2019.01.217

Streptozocin (STZ) is a broad range antibiotic, highly genotoxic, antineoplastic and hyperglycemic. HSA is the most abundant protein in physiology and it binds to almost all exogenic and endogenic ligands, including drugs. STZ-induced fluorescence quenching of HSA has been done at pH 7.4, pH 3.5 and at pH 7.4 with 4.5 M urea at temperatures 286 K, 291 K, and 306 K. Ksv found to be 103 M-1, binding constant 1.5X103M-1 and binding sites ~1. But, Ksv for HSA and glucopyranose interaction was found lesser than that of HSA-STZ binding. Binding of STZ/glucopyranose on HSA seems to result in complex formation as calculated Kq > 1010 M-1 s-1. The number of binding sites, binding constants, and binding energies were increased with temperature. The ΔG0, ΔH0, and ΔS0 for HSA-STZ interaction were found to be -17.7 × 103 J·mol-1; 2.34 × 105 J·mol-1 and 841 JK-1 mol-1 respectively at pH 7.4 and 291 K. The comparative bindings of N, F and I states of HSA with STZ and their molecular docking analyses indicate that IIIA-B junction (i.e., inter-helix h6DOM3-h7DOM3) is the probable binding site, a locus close to fatty acid binding site-5. These results could be useful for therapeutic and analytical exploitation of STZ, as albumin used as the vehicle for drug delivery.

Streptozocin; a GLUT2 binding drug, interacts with human serum albumin at loci h6 DOM3-h7 DOM3

Int J Biol Macromol2019 May 1;128:923-933.PMID: 30716368DOI: 10.1016/j.ijbiomac.2019.01.217

Streptozocin (STZ) is a broad range antibiotic, highly genotoxic, antineoplastic and hyperglycemic. HSA is the most abundant protein in physiology and it binds to almost all exogenic and endogenic ligands, including drugs. STZ-induced fluorescence quenching of HSA has been done at pH 7.4, pH 3.5 and at pH 7.4 with 4.5 M urea at temperatures 286 K, 291 K, and 306 K. Ksv found to be 103 M-1, binding constant 1.5X103M-1 and binding sites ~1. But, Ksv for HSA and glucopyranose interaction was found lesser than that of HSA-STZ binding. Binding of STZ/glucopyranose on HSA seems to result in complex formation as calculated Kq > 1010 M-1 s-1. The number of binding sites, binding constants, and binding energies were increased with temperature. The ΔG0, ΔH0, and ΔS0 for HSA-STZ interaction were found to be -17.7 × 103 J·mol-1; 2.34 × 105 J·mol-1 and 841 JK-1 mol-1 respectively at pH 7.4 and 291 K. The comparative bindings of N, F and I states of HSA with STZ and their molecular docking analyses indicate that IIIA-B junction (i.e., inter-helix h6DOM3-h7DOM3) is the probable binding site, a locus close to fatty acid binding site-5. These results could be useful for therapeutic and analytical exploitation of STZ, as albumin used as the vehicle for drug delivery.

Renal function in patients receiving streptozocin for locally advanced or metastatic digestive neuroendocrine tumours: results of the Streptotox-FFCD 0906 study

Clin Res Hepatol Gastroenterol2021 Sep;45(5):101572.PMID: 33751987DOI: 10.1016/j.clinre.2020.10.014

Introduction: Streptozocin can impair renal function. The purpose of this study was to evaluate the evolution of renal function in patients receiving this anti-mitotic for the treatment of locally advanced/metastatic digestive well differentiated neuroendocrine tumours.
Methods: A prospective and a retrospective cohort of patients with normal baseline renal function were analysed. The primary endpoint was the incidence of a decrease in the estimated glomerular filtration rate ≥ 25% during treatment. Secondary endpoints were the evaluation of glomerular filtration rate changes, the impact of combined nephrotoxic treatments, other toxicities, compliance, and the objective response rate.
Results: After screening 142 patients, 27 were included in the prospective and 84 in the retrospective cohort. A decrease in estimated glomerular filtration rate ≥ 25% was observed in 32 patients (30%): respectively four (15.4%) and 28 patients (34.1%) among respectively 26 and 82 patients with numerous measures (P = 0.0097). Altogether, 39 patients (35%) experienced grade 1-2 renal toxicity, while no grade 3-4 occurred in the prospective and 1 occurred in the retrospective cohort. Renal toxicity was more frequent in the retrospective cohort with a less careful follow up. As best responses, objective response was achieved in 27% of patients with pancreatic primary tumours, disease control in 78.9% of patients with pancreatic primary tumours, in 87% of those with small bowel tumours and in 72.7% of patients with other primary locations.
Conclusions: Strongly recommended for pancreatic NET, streptozocin is associated with frequent mild renal toxicity but low occurrence of renal impairment in patients with baseline normal renal function and under adequate hydration.

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