Lupeol-Fagarasterol-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELupeolCat. No.: HY-N0790CAS No.: 545-47-1Synonyms: Fagarasterol分式: CHO分量: 426.72作靶點(diǎn): Androgen Receptor作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (14.06 mM; Need ultr

2、asonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3435 mL 11.7173 mL 23.4346 mL5 mM 0.4687 mL 2.3435 mL 4.6869 mL10 mM 0.2343 mL 1.1717 mL 2.3435 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Lupeol種新型雄激素受體抑制劑。IC50 & Target Androgen receptor 1體外研究Lupeol,

3、an effective AR inhibitor, can be developed as a potential agent to treat human prostate cancer(CaP). Lupeol (1050 M) treatment for 48 h results in a dose-dependent growth inhibition of androgen-1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEdependent phenotype (ADPC) cells viz., LAPC4 and LNCaP c

4、ells with an IC50 of 15.9 and 17.3 M,respectively. Lupeol also inhibits the growth of 22R_1 with an IC50 of 19.1 M. Further, Lupeol inhibits thegrowth of C4-2b cells with an IC50 of 25 M. Lupeol has the potential to inhibit the growth of CaP cells ofboth ADPC and CRPC phenotype. Androgens by activat

5、ing AR are known to drive the growth of CaP cells1.體內(nèi)研究 Lupeol is an effective agent that has the potential to inhibit the tumorigenicity of CaP cells in vivo. At theconclusion of the study on day 56, the total circulating serum-PSA levels (secreted by the implanted tumorcells) are measured. At 56th

6、day post-implantation, PSA levels are observed between 11.95-12.79 ng/mL incontrol animals with LNCaP-tumors and C4-2b-tumors, respectively. However, Lupeol-treated counterpartanimals exhibits reduced serum-PSA levels in a range of 4.25-7.09 ng/mL. Tumor tissues of animalsreceiving Lupeol treatment

7、exhibits reduced serum-PSA levels as compared to control 1.PROTOCOLCell Assay 1 LAPC4 (wild-functional AR/ADPC); LNCaP (mutant-functional AR/ADPC); 22R1 (mutant-functionalAR/androgen-independent but responsive); C4-2b cells (mutant-functional AR/CRPC) and PC-3 and DU-145(lack of endogenous AR) are g

8、rown under standard cell culture conditions at 37C and 5% CO2 environment.The cells (60-70% confluent) are treated with Lupeol (10-50 M) for 48 h in complete growth medium. Forcombination set of experiments, cells are treated with either agonistic androgen-analogue R1881 (1 nM), orantagonist Bicalut

9、amide (10 M), and/or combination (R1881+Lupeol) for 48 h. After incubation for specifiedtimes at 37C, MTT assay is performed. For sensitization studies, hormone refractory C4-2b cells are treatedwith Lupeol for 24 h. After 24 h, cells are incubated with Bicalutamide (10 M) for further 24 h. Cells ar

10、eassessed for viability 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Tumor studies are conducted in athymic nude mice and two cohorts of animals are created. 3106 of cellsare injected subcutaneously in the right flanks

11、 of each mouse. Each cohort receive a specific cell type eitherLNCaP or C4-2b. One week post-implantation, twenty mice (with visible tumors) in each cohort are randomlydivided into two groups, with 10 animals in each group. The first group of animals receive intraperitoneal (i.p.)administration of c

12、orn oil (100 L) and served as control. The second group of animals receive i.p.administration of Lupeol (40 mg/kg in 100 L of corn oil) three times/week. Body weights and tumor volumesare recorded. All animals of group 1 and group 2 are sacrificed when tumors cross a pre-set endpoint volumeof 1,000

13、mm3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Siddique HR, et al. Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy. Clin Cancer Res. 2011 Aug15;17(16):5379-91.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.Me