维莫德吉作用机制 - Medchemexpress - MCE中国

1、Product Data SheetVismodegibCat. No.: HY-10440CAS No.: 879085-55-9分式: CHClNOS分量: 421.3作靶点: Hedgehog; Autophagy作通路: Stem Cell/Wnt; Autophagy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 DMSO : 50 mg/mL (118.68 mM)Ethanol : 2.86 mg/mL (6.79 mM; Need ultrasonic)H2O : 4

2、6 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts4.PROTOCOLCell Assay 2 When MTT assay is performed, an MTT reagent is added to each well to a final concentration of 150 g/mL, and thecells are incubated for 1 to 2 hours at 37C. The medium is then replaced with DMSO to disso

3、lve the reactionproduct. Absorbance at 570 nm is quantified using a spectra MAX 340pc plate reader. For the XTT assay, 1 mg/mLXTT is mixed with 0.025 mM PMS, and 50 L of the mixture is added to each well and incubated for 4 hours at 37C.After the plates are mixed on a plate shaker, absorbance at 450

4、 nm is measured. All results are normalized to apercentage of absorbance obtained in controls.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Tumor-bearing mice are distributed into tumor volume-matched cohorts when the tumors reache between 200

5、andAdministration 2 350 mm3. The vismodegib-resistant medulloblastoma allograft, sg274, is developed by intermittent suboptimaldosing of a Ptch+/, p53/medulloblastoma allograft. Vismodegib is formulated as a suspension in 0.5% methyl-cellulose, 0.2% tween-80 (MCT), and is administered orally. Tumor

6、volumes are determined using digital calipersusing the formula (LWW)/2. Tumor growth inhibition (%TGI) is calculated as the percentage of the area under thefitted curve (AUC) for the respective dose group per day in relation to the vehicle, such that %TGI=1001-(AUCtreatment/day)/(AUCvehicle/day).MCE

7、 has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献Page 2 of 3 www.MedChemE J Control Release. 2019 Apr 17;303:77-90. Oncogene. 2020 May 14. Oncogene. 2020 Feb. Cancer Lett. 2018 Apr 28;420:195-207. Oncogenesis. 2018 Mar 13;7(3):24.See more custome

8、r validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Scales SJ, et al. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009, 30(6), 303-312.2. Zhang Y, et al. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP

9、 and ABCB1/Pgp. Neoplasia. 2009, 11(1), 96-101.3. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in NSC 119875-resistant lungcancer cells. Anticancer Res. 2012, 32(1), 89-94.4. Wong H, et al. Pharmacokinetic-pharmacodynamic analy

10、sis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathwayactivation. Clin Cancer Res. 2011, 17(14), 4682-4692.5. Elhenawy AA, et al. Possible antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor, in mice model of Schistosoma-induced liverfibrosis. Parasitol Int. 2017 Oct;66(5):545-554.6. Ma W, et al. Reduced Smoothened level rescued A-induced memory deficits and neuronal inflammation in animal models of Alzheimers disease. JGenet Genomics. 2018 May 20;45(5):237-246.McePdfHeightCaution: Product has not been fully validated for