盐酸RGX-104 T5128

Product Introduction
Bioactivity


英文名: RGX-104 hydrochloride

描述: RGX-104 hydrochloride (SB742881) 是小分子LXR 激动剂，利用 ApoE 基因的转录激活，调节先天免疫。

细胞实验: Myeloid-derived suppressor cells were isolated as previously described from splenic tissue of tumor-bearing mice. One hundred thousand cells were plated in quadruplicates in poly-L-lysine coated plates. After 3 hours of treatment with 1uM RGX-104 or DMSO as vehicle, cells were fixed with 4% PFA for 15 minutes and wash 3 times with 1X PBS prior staining. Rabbit monoclonal anti-Ki67 antibody (1:400 dilution) was applied at 4C overnight. Cells were incubated with Alexa Fluor 488 secondary antibody (1:200 dilution) for one hour at room temperature, counterstained with DAPI (1:1000 dilution) and mounted with Prolong Gold. For the analysis of the percentage of Ki67 positive cells, five fields from each replicate were imaged at 20x magnification using Zeiss Axio Imager fluorescence microscope.

动物实验: For MDSC adoptive transfer experiments into tumor-bearing mice, 2 × 10^6 MDSCs were isolated as described above from C57BL/6 tumor-bearing mice and subsequently labeled with BD Horizon Violet (BV) Proliferation Dye and then adoptively transferred via retro-orbital injection into wild-type mice. Mice were then treated with RGX-104 (100 mg/kg/day) or control diet for 36 hours. Spleens of recipient mice were then harvested and processed for flow cytometry analysis as described above. For MDSC adoptive transfer experiments in to WT and ApoE?/? non-tumor bearing mice, 5 × 10^6 MDSCs were isolated as described above from tumor-bearing mice (either wild-type C57BL/6 or Apoe?/? mice) and subsequently labeled with BV cell tracker dye and then adoptively transferred via retro-orbital injection into either wild-type or Apoe?/? mice. Mice were then treated with GW3965 (100 mg/kg/day) or control diet for 48 hours. Spleens of recipient mice were then harvested and processed for flow cytometry analysis.

体内活性: Oral administration of RGX-104 to animals bearing palpable tumors significantly suppressed the growth of multiple cancer types. Strong tumor growth suppression was also observed in animals bearing large tumors. As compared to controls after 8 days of treatment, apoptotic circulating G-MDSCs of total CD45+ lymphocytes in RGX-104-treated (100 mg/kg) mice had a significant increase.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 115 mg/mL (181.81 mM)


关键字: RGX 104 Hydrochloride | inhibit | LXR | RGX-104 | RGX 104 | RGX104 Hydrochloride | SB-742881 | RGX-104 Hydrochloride | RGX 104 hydrochloride | RGX104 hydrochloride | Inhibitor | SB 742881 | RGX104 | Liver X receptor

相关产品: BMS-779788 | GAC0003A4 | GSK2033 | 24-Hydroxycholesterol | 27-Hydroxycholesterol | GW3965 hydrochloride | Ethyl 2,4,6-trihydroxybenzoate | Licochalcone E | GSK3987 | LXR-623

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Nuclear Receptor Compound Library | Anti-Cancer Active Compound Library | Lipid Metabolism Compound Library | Bioactive Compound Library

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