Bleomycin-sulfate _DNA Synthesis 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBleomycin sulfateCat. No.: HY-17565CAS No.: 9041-93-4分式: CHNOS分量: 1512.62作靶点: DNA/RNA Synthesis; Bacterial作通路: Cell Cycle/DNA Damage; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、H2O : 255 mg/mL (168.58 mM; Need ultrasonic and warming)DMSO : 16.67 mg/mL (11.02 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.6611 mL 3.3055 mL 6.6110 mL5 mM 0.1322 mL 0.6611 mL 1.3222 mL10 mM 0.0661 mL 0.3306 mL 0.6611 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLO

3、GICAL ACTIVITY物活性 Bleomycin sulfate是具有有效抗肿瘤活性的DNA合成抑制剂。IC50 & Target DNA/RNA Synthesis 1体外研究Bleomycin (BLM) is chosen as the best-studied micronucleus (MN) inducers in human lymphocytes withdifferent mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and1/3 Master

4、 of Small Molecules 您边的抑制剂师www.MedChemEdouble strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimeticcompound, resembling almost completely the genetic effect of ionizing radiation 1. The IC50 value ofBleomycin sulfate for UT-SCC-19A cell line is 4.01.3 n

5、M. UT-SCC-12A and UT-SCC-12B are both moreresistant to Bleomycin (BLM); IC50 values are 14.22.8 nM and 13.01.1 nM, respectively 2. Bleomycin(BLM) induces a significant increase in the percentage of aberrant cells (i.e., cells showing at least oneaberration) and in the frequency of chromosomal aberra

6、tions per cell compare with control cultures 18 h aftertreatment (p 3.体内研究 A short-range beta-emitting radionuclide combined to Bleomycin (In-111-BLMC) is a tumor-targeting agent inSCCs. Within 35 days the weight of nude mice increases 2.80.6g. At 25 and 35 days after tumorinoculations the tumor vol

7、umes are 11151 mm3 and 874577 mm3, respectively. The calculated doublingtime is 3.860.76 days. SCC cell lines demonstrate different sensitivity to Bleomycin. Our SCC tumorxenograft model shows a rapid growth proper for radiochemotherapeutic studies using In-111-BLMC. Theuptake of In-111-BLMC in vivo

8、 has been directly proportional to proliferation activity, and the tumors with highbinding capacity could be predicted from animal model dose calculations 2. At 7 and 14 days afterBleomycin (BLM) treatment, the signal of TGF-1 is significantly stronger than that of the control group. At 28days after

9、 treatment, the TGF-1 signal became a little weaker. At 7 and 14 days of Bleomycin plus Dexgroup, the signal of TGF-1 is also stronger than that of the control group. However, at 28 days, the TGF-1signal become weaker and is a little stronger than the level of control group. All the results are give

10、n bycomparison of the average IOD value 4.PROTOCOLCell Assay 3 ADIPO-P2 cells are grown in D-MEM high glucose medium supplemented with 20% fetal calf serum,penicillin (100 U/mL) and streptomycin (100 g/mL) at 37C and 5% CO2 atmosphere. Cells are cultured asmonolayer in TC25 Corning flasks containing

11、 1.5105 cells/mL. For each experiment, two flasks are set up,one for the control and one for the treated culture. During the log phase of growth ADIPO-P2 cells are treatedwith a 30 min pulse of 2.5 g/mL of Bleomycin (dissolved in sterile 0.9% NaCl). Control cultures are set up inparallel but not exp

12、osed to Bleomycin. At the end of the pulse treatment with Bleomycin, the cells are washedtwice with Hanks balanced salt solution and kept in culture with fresh culture medium until harvesting. Cellsare continuously maintained in culture during 5 passages or subcultures after treatment. Subcultivatio

13、n iscarried out whenever the cultures became confluent (approximately 4105 cells/mL of culture medium). Toestimate cell growth, at the time of subcultivation cells are collected by trypsinization, an aliquot of about 200L stained with 0.4% trypan blue, and the number of viable cells (cells not stain

14、ed) is determined 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 4Administration 4 60 CD-1 mice are randomly divided into the following 3 groups (n=20 each): saline-water; Bleomycin -water;Bleomycin plus Dexamethasone (Dex). Mice in the s

15、aline group are injected intratracheally with 2 mL/kgsaline; the others are injected intratracheally with Bleomycin (5 mg/kg, 2 mL/kg in saline). Twenty-four hoursafter Bleomycin treatment, mice are given by gavage 0.45 mg/kg/d DEX. The day of intratracheal injectionwith Bleomycin or saline is desig

16、nated day 0.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 ACS Appl Mater Interfaces. 2019 Jan 16;11(2):1942-1950. Am J Respir Cell Mol Biol. 2019 Apr;60(4):478-487. Mutat Res Genet Toxicol E

17、nviron Mutagen. 2016 Sep 15;808:27-37.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by mitomycin C andbleomycin in human leukocytes. Mol Cytogenet. 2016 Jun 21;9:49.2. Jaas

18、kela-Saari HA, et al. Squamous cell cancer cell lines: sensitivity to bleomycin and suitability for animal xenograft studies. ActaOtolaryngol Suppl. 1997;529:241-4.3. Paviolo NS, et al. Telomere instability is present in the progeny of mammalian cells exposed to bleomycin. Mutat Res. 2012 Jun 1;734(1-2):5-11.4. Shi K, et al. Dexamethasone attenuates bleomycin-induced lung fibrosis in mice through T