"目录号: HY-13753
Cell Cycle/DNA Damage-
Streptozocin 是一种有效的DNA甲基化试剂，作用于 HL60，K562 和 C1498 细胞，IC50分别为 11.7，904 和 1024 μg/mL。
DNA/RNA SynthesisDNA Alkylator/Crosslinker
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生物活性
Description
Streptozocin is a potentDNA-methylatingagent, withIC50values of 11.7, 904 and 1024 μg/mL for HL60, K562 and C1498 cells respectively.
IC50& Target
DNA alkylator[1]
In Vitro
Streptozocin (STZ) shows higher cytotoxic effect in vitro on hematological cell lines compared to Alloxan (ALX). ALX appeares not to be toxic for the studied cell lines with estimated IC50values of 2809, 3679 or over 4000 μg/mL for HL60, K562 and C1498 cells, respectively. Streptozocin is more toxic, especially for the human myeloid leukemia cell line, HL60. The IC50values of Streptozocin are 11.7, 904 and 1024 μg/mL for HL60, K562 and C1498 cells, respectively. Results also show that the murine leukemic cells are more resistant to Streptozocin and ALX cytotoxicity than human leukemic cells[2].
In Vivo
Streptozocin (STZ)-injected mice show tendency to have lower body weight than that observed in animals injected with ALX. Streptozocin -injected mice have significantly fewer splenocytes (22.2±3.2×106; n=10) compared to mice injected with ALX (60.7±4.3×106; n=15; p=0.01)[2].
Clinical Trial
NCT00609765
H. Lee Moffitt Cancer Center and Research Institute-Genentech, Inc.
Pancreatic Cancer
August 2007
Phase 2
NCT00602082
Cambridge University Hospitals NHS Foundation Trust-National Cancer Institute (NCI)
Gastrointestinal Carcinoid Tumor-Islet Cell Tumor
August 2005
Phase 2
NCT00004688
Emory University-FDA Office of Orphan Products Development
Anaplastic Astrocytoma-Anaplastic Oligodendroglioma-Mixed Gliomas-Glioblastoma Multiforme-Recurrent Brain Tumor
August 1996
Phase 2
NCT00003543
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)
Colorectal Cancer
June 1998
Phase 1
NCT00001165
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)-National Institutes of Health Clinical Center (CC)
Islet Cell Adenoma-Neoplasm Metastasis-Zollinger Ellison Syndrome
September 1978
Phase 2
NCT00094497
Collaborative Group for Adrenocortical Carcinoma Treatment-German Federal Ministry of Education and Research-National Cancer Institute (NCI)
Carcinoma, Adrenal Cortical
June 2004
Phase 3
NCT00448136
Hoffmann-La Roche
Neoplasms
July 2007
Phase 2
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References
[1].Bennett RA, et al. Alkylation of DNA in rat tissues following administration of streptozotocin. Cancer Res. 1981 Jul;41(7):2786-90.
[2].Diab RA, et al. Immunotoxicological effects of streptozotocin and alloxan: in vitro and in vivo studies. Immunol Lett. 2015 Feb;163(2):193-8.
[3].Acer S, et al. Oxidative stress of crystalline lens in rat menopausal model. Arq Bras Oftalmol. 2016 Jul-Aug;79(4):222-5.