ADPM06 T40575

Product Introduction
Bioactivity


英文名: ADPM06

描述: ADPM06, an azadipyrromethene compound, is a new nonporphyrin photodynamic therapeutic (PDT) agent with potential as a lead candidate. It demonstrates significant IC50 values in the micro-molar range in human tumor cells, as well as inducing apoptosis.

体外活性: The efficacy of ADPM01 is completely ablated at a 1% oxygen level in Hela and MRC5 cell lines. ADPM06 displays only a partial reduction in light-induced activity in hypoxic as compared to normoxic conditions[1]. ADPM06-PDT induces ER stress and unfolded protein response[2]. ADPM06-PDT induces apoptosis and involves caspase enzymatic activity[2]. Following ADPM06-PDT, a rapid processing of XBP1 mRNA occurs resulting in the removal of an intron from the mRNA in a spliceosome-independent manner, a post-transcriptional modification catalyzed by the action of activated inositol-requiring protein 1 (IRE1)[2]. ADPM06-PDT-induced apoptosis involves the generation of ROS[2]. Cell Viability Assay[1]Cell Line: Hela and MRC5 cell lines. Concentration: 1 nM - 100μM. Incubation Time: 24 h. Result: Retained considerable efficacy, with EC 50 values of 1.5 and 1.6 × 10 ?6 M for HeLa and MRC5 cells, respectively.

体内活性: ADPM06-PDT has revealed an initiation of apoptosis in vivo, as well as induction of an ER stress response[2]. ADPM06-PDT is well tolerated in vivo and elicits impressive complete response rates in various models of cancer when a short drug-light interval is applied[2]. Animal Model: Female Balb C nu/nu mice[2]. Dosage: 2 mg/kg in 0.3 mL solution via the lateral tail vein. Administration: IV. Result: Revealed a rapid reduction in tumor-specific luciferase activity as early as 1-hr post-PDT, with levels decreasing further 4-hr post-PDT.

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

关键字: ADPM06 | ADPM 06 | ADPM-06

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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