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    Streptozotocin (STZ)
    Streptozotocin (STZ)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1856
    CAS #: 18883-66-4Purity ≥98%

    Description: 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 a methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozocin is a methylnitrosourea antineoplastic antibiotic isolated from the bacterium Streptomyces achromogenes. Streptozocin alkylates DNA, forming inter-strand DNA cross-links and inhibiting DNA synthesis. Due to its glucose moiety, this agent is readily taken up by pancreatic beta cells, inducing diabetes mellitus at high concentrations. 

    References: Mutat Res. 2002;512:121-34; Biochem Mol Biol Int. 1996;39(6):1229-36; Diabetes. 1967;16(1):51-6.

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    Molecular Weight (MW)265.22 
    CAS No.18883-66-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (199.8 mM) 
    Water: 53 mg/mL (199.8 mM) 
    Ethanol: <1 mg/mL
    Solubility (In vivo)Saline: 30 mg/mL
    SynonymsNSC-85998; U9889; U-9889; U 9889; NCI-C03167; NSC-85998; AI3-50821; NRRL 2697; STZ; SZC; SZN; Zanosar.

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    In Vitro

    In vitro activity: Streptozotocin directly methylates DNA and is highly genotoxic, producing DNA strand breaks, alkali-labile sites, unscheduled DNA synthesis, DNA adducts, chromosomal aberrations, micronuclei, sister chromatid exchanges, and cell death. Free radicals are involved in the production of DNA and chromosome damage by Streptozotocin. Streptozotocin is toxic to pancreatic beta cell. Exposed to 15 mM Streptozotocin for 1 hr followed by a 24 hrs recovery period induces apoptosis in murine pancreatic beta cell line, INS-1. Streptozotocin (30 mM) causes the cells to undergo necrosis (22%) as well as apoptosis (17%).

    Kinase Assay: Streptozocin is a potent DNA-methylating agent, with IC50s of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells respectively.

    Cell Assay: Human and murine cell lines are cultured in triplicate in 96-well plates at a density of 2×104 cells/well in the absence (untreated control) or presence of various concentrations of ALX (20-3000 μg/mL) or STZ (1-3000 μg/mL) for 48 h at 37°C under a humidified atmosphere containing 5% CO2. Cells incubated in complete media including dH2O in a final concentration of 0.1% served as control for solvent toxicity and cells incubated in complete medium are used as a control for the experiments. The effects of the tested drugs on tumor cell growth or viability are determined employing the MTT assay in accordance with the manufacturer's instructions. The IC50values (drug concentration that induces 50% inhibition of the cell growth) are calculated using the GraphPad Prism 4 program.

    In VivoStreptozotocin is often used to induce diabetes mellitus in experimental animals. Streptozotocin is selectively accumulated in pancreatic beta cells via the low-affinity GLUT 2 glucose transporter. Streptozotocin (60 mg/kg) injection for 4 month induces rapid degranulation of beta cells without necrosis, development of cataracts and accumulation of glycogen in the proximal convoluted tubules of the kidney. Streptozotocin (100 mg/kg) produces lesions in the exocrine cells of the pancreas, and persistence of small, possibly secretory, granules in the Golgi zone of beta cells in rats of ‘Streptozotocin diabetes’. Streptozotocin is found to be carcinogenic in rats, mice and hamster. A single administration of Streptozotocin is able to induce tumors in kidney, liver, lung, pancreas, uterine and liver tumors in hamster. Intraperitoneally injected with Streptozotocin (100-150 mg/kg) for normotensive Wistar Kyoto rats (WKY) for 12 months induces carcinogenesis with tumors incidence of 70% in liver, 20% in kidney and 10% in liver and kidney.  
    Animal model Mice and rats
    Formulation & DosageMice: Male C57BL/6 mice (10-16 weeks) are used.The age group distribution in the mouse group treated with Streptozocin and ALX as well as controls is as follows: Streptozocin xenograft (n=7, median age 14 weeks), ALX xenograft (n=11, median age 15 weeks), Streptozocin non-transplanted (n=7, median age 14 weeks), ALX non-transplanted (n=15, median age 15 weeks).Male C57BL/6 mice are under inhalation anesthesia injected via the penile vein with ALX (75 mg/mL) or Streptozocin (180 mg/kg). Control group contain male C57BL/6 mice. Blood glucose levels and body weight are measured before injection, after 6 h, then daily after drug injection; 

    Rats: Thirty rats underwent oophorectomy to induce menopausal status. Oophorectomy is performed under sterile conditions via a midline incision after anesthetization using intraperitoneal injection of ketamine hydrochloride (90 mg/kg) and xylazine (10 mg/kg). The incisions are closed with 3.0 polyglactin sutures. The remaining 10 rats formed the control group (Group 1). Ten of the 30 rats that underwent oophorectomy constituted the menopause control group (Group 2). Beginning 1 week after the operation, methylprednisolone (1 mg/kg) is injected daily until the end of the study to mimic steroid treatment for rheumatologic diseases in 10 rats (Group 3). Group 4 consisted of rats that received intraperitoneal administration of Streptozocin (50 mg/kg) to induce diabetes mellitus (DM) 1 week after the oophorectomy. Blood glucose level is checked 3 days after Streptozocin administration, and values >250 mg/dL are considered as positive for DM.

    ReferencesMutat Res. 2002 Dec;512(2-3):121-34; Biochem Mol Biol Int. 1996 Aug;39(6):1229-36; Diabetes. 1967 Jan;16(1):51-6. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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