Verteporfin-CL-318952-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVerteporfinCat. No.: HY-B0146CAS No.: 129497-78-5Synonyms: CL 318952分式: CHNO分量: 718.79作靶點(diǎn): YAP; Autophagy作通路: Stem Cell/Wnt; Autophagy儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性

2、數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 8 mg/mL (11.13 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.8 mg/mL (1.11 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.8 mg/mL (1.11 mM); Suspended solution; Need ultrasonic and warming1/3 Master of Small Molecules 您邊的抑制劑

3、師www.MedChemEBIOLOGICAL ACTIVITY物活性 Verteporfin種于光動療法的光敏劑，于消除與年齡相關(guān)的 斑變性等疾病相關(guān)的眼內(nèi)異常管。Verteporfin 種 YAP 抑制劑，可破壞YAP-TEAD相互作。體外研究 Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition(GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, re

4、spectively, whereas GI50 for ALL-1,TCC-Y/sr, and NPhA1 are 3.93 M, 2.11 M, and 5.61 M, respectively. GSH significantly reduces thesensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential inPDX cells 1. Verteporfin reduces the PTX-resistance on HCT-

5、8/T cells by inhibiting YAP expression andcombination therapy with verteporfin and paclitaxel (PTX) shows synergism on inhibition of YAP andcytotoxicity to HCT-8/T 2.體內(nèi)研究 Verteporfin (10 mg/kg, c.s.c.) and dasatinib significantly reduces the leukemia cell ratio, and combinedtherapy further reduced t

6、he number of leukemia cells in the spleen 1.PROTOCOLCell Assay 1 PDX cells co-cultured with S17 cells are treated with 16 combinations of verteporfin (60 nM, 120 nM, 180 nM,and 240 nM) and dasatinib (12 nM, 24 nM, 36 nM, and 48 nM). The viabilities of cells treated with eachcombination are measured

7、after 48 h using FACS Aria flow cytometer. In order to estimate drug interactionbetween verteporfin and dasatinib, a normalized isobologram and fraction affectedcombination index (CI) plotare made using CompuSyn software. CI values greater than 1.0 indicated antagonistic effects, equal to 1.0additiv

8、e effects, and below 1.0 synergistic effects.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: PhLO cells (1.0107/mouse) are injected intravenously into 6-week-old male NOG mice, which areAdministration 1 then treated with vehicle, verteporfi

9、n (140 mg/kg/day), dasatinib (20 mg/kg/day), and a combination of thesedrugs from days 22 to 28. Verteporfin is administered by continuous subcutaneous infusion (c.s.c.) usingAlzet osmotic pumps. An intraperitoneal injection (i.p.) is performed for dasatinib. All mice are sacrificed onday 28 and the

10、 chimerism of leukemia cells is investigated by flow cytometer using an anti-human CD19antibody and antimouse CD45 antibody. Blood concentrations of verteporfin are calculated by LCMS-2020.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Mol

11、Cell. 2019 Jan 3;73(1):7-21.e7. EMBO Mol Med. 2018 Nov;10(11). pii: e8699. Cell Syst. 2018 Apr 25;6(4):424-443.e7. J Dent Res. 2019 Jul;98(8):920-929. Front Cell Neurosci. 2018 Dec 11;12:489.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREF

12、ERENCES1. Morishita T, et al. The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblasticleukemia and synergistically works with dasatinib. Oncotarget. 2016 Aug 2.2. Pan W, et al. Verteporfin can Reverse the Paclitaxel Resistance Induced by YAP Over-Expression in HCT-8/T Cells withoutPhotoactivation through Inhibiting YAP Expression. Cell Physiol Biochem. 2016;39(2):481-90.McePdfHeightCau