化合物 CCT251236 T14905

Product Introduction
Bioactivity


英文名: CCT251236

描述: CCT251236 is an orally available Pirin ligand obtained from a heat shock transcription factor 1 (hsf1) phenotypic screen. It inhibits HSF1-mediated HSP72 induction (IC50: 19 nM).

体外活性: CCT367766 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72, and HSP27 expression as a concentration manner in SK-OV-3 cells. CCT367766 blocks the induction of HSPA1A mRNA by 17-AAG in a dose-dependent manner. CCT367766 (0-100 nM; 24hours) displays the desired balance of in vitro properties while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC50: 19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI50?is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay. CCT367766 (0-100 nM; 24 hours) pre-treated with 250 nM 17-AAG for 6h.

体内活性: CCT367766 (p.o.; 20 mg/kg; 33 days) has a clear therapeutic efficacy in mice with a tumor growth inhibition (%TGI) of 70% based on final tumor volumes. After 33 days, the mean tumor weights decrease 64% when compares to the control group. In addition, the compound's basicity and the high volume of the distribution shown in tumors with tumor concentrations of?CCT367766?as high as 940 nM. CCT367766 (p.o.; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free?Cav0–24h?value of 2.0 nM and 1.2 nM, respectively [2].

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 150 mg/mL (271.43 mM)


关键字: CCT-251236 | CCT 251236 | CCT251236

相关产品: Zelavespib hydrochloride | VER-82576 | Tanespimycin | TRC051384 | Ethoxyquin | Eupalinolide A | HSP70-IN-1 | YUM70 | Alvespimycin | Chetomin

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途