产品
编 号:F368350
分子式:C34H24BBr2F2N3O2
分子量:715.19
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5mg
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10mg
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25mg
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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.

体内研究:
ADPM06-PDT has revealed an initiation of apoptosis in vivo, as well as induction of an ER stress response.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.Animal Model:Female Balb C nu/nu mice.
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.

体外研究:
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.ADPM06-PDT induces ER stress and unfolded protein response.ADPM06-PDT induces apoptosis and involves caspase enzymatic activity.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).ADPM06-PDT-induced apoptosis involves the generation of ROS.
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