ADPM06

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ADPM06 

ADPM06,是一种氮唑吡咯甲基,是可用于光动力治疗 (PDT) 的化合物。ADPM06 在人肿瘤细胞系中显示较好的活性,并可诱导凋亡 (apoptosis)

ADPM06

ADPM06 Chemical Structure

CAS No. : 490035-90-0

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生物活性

ADPM06, a lead candidate azadipyrromethene, is a novel nonporphyrin photodynamic therapeutic (PDT) agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis[1].

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hela and MRC5 cell lines.
Concentration: 1 nM – 100μM.
Incubation Time: 24 h.
Result: Retained considerable efficacy, with EC50 values of 1.5 and 1.6 × 10−6 M for HeLa and MRC5 cells, respectively.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

715.19

Formula

C34H24BBr2F2N3O2

CAS 号

490035-90-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. W M Gallagher, et al. A potent nonporphyrin class of photodynamic therapeutic agent: cellular localisation, cytotoxic potential and influence of hypoxia. Br J Cancer. 2005 May 9; 92(9): 1702-1710.

    [2]. Aisling E O’Connor, et al. Mechanism of cell death mediated by a BF2-chelated tetraaryl-azadipyrromethene photodynamic therapeutic: dissection of the apoptotic pathway in vitro and in vivo. Int J Cancer. 2012 Feb 1;130(3):705-15.

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