ADPM06
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 95.0%
- CAS No.: 490035-90-0
- Formula: C34H24BBr2F2N3O2
- Molecular Weight:715.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>50 μM
Compound: 1; ADPM06
|
Dark toxicity in human HeLa cells assessed as reduction in cell viability after 3 hrs by MTT assay
Dark toxicity in human HeLa cells assessed as reduction in cell viability after 3 hrs by MTT assay
|
[PMID: 32787080] |
| HeLa | IC50 |
0.13 μM
Compound: 1; ADPM06
|
Phototoxicity against human HeLa cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
Phototoxicity against human HeLa cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
|
[PMID: 32787080] |
| HeLa | IC50 |
41.7 μM
Compound: BDP-4
|
Dark cytotoxicity against human HeLa cells assessed as inhibition of cell viability incubated for 3 hrs by CCK8 assay
Dark cytotoxicity against human HeLa cells assessed as inhibition of cell viability incubated for 3 hrs by CCK8 assay
|
[PMID: 39167079] |
| HeLa | IC50 |
64.2 nM
Compound: BDP-4
|
Phototoxicity against human HeLa cells assessed as inhibition of cell viability preincubated for 3 hrs followed by photo-irradiation of 54 J/cm2 for 24 hrs by CCK8 assay
Phototoxicity against human HeLa cells assessed as inhibition of cell viability preincubated for 3 hrs followed by photo-irradiation of 54 J/cm2 for 24 hrs by CCK8 assay
|
[PMID: 39167079] |
| MCF7 | IC50 |
>50 μM
Compound: 1; ADPM06
|
Dark toxicity in human MCF7 cells assessed as reduction in cell viability after 3 hrs by MTT assay
Dark toxicity in human MCF7 cells assessed as reduction in cell viability after 3 hrs by MTT assay
|
[PMID: 32787080] |
| MCF7 | IC50 |
0.15 μM
Compound: 1; ADPM06
|
Phototoxicity against human MCF7 cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
Phototoxicity against human MCF7 cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
|
[PMID: 32787080] |
| SW480 | IC50 |
>50 μM
Compound: 1; ADPM06
|
Dark toxicity in human SW480 cells assessed as reduction in cell viability after 3 hrs by MTT assay
Dark toxicity in human SW480 cells assessed as reduction in cell viability after 3 hrs by MTT assay
|
[PMID: 32787080] |
| SW480 | IC50 |
0.16 μM
Compound: 1; ADPM06
|
Phototoxicity against human SW480 cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
Phototoxicity against human SW480 cells assessed as reduction in cell viability preincubated for 3 hrs followed by 54 J/cm2 light irradiation and measured after 24 hrs by MTT assay
|
[PMID: 32787080] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hela and MRC5 cell lines.
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Concentration:1 nM - 100μM.
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Incubation Time:24 h.
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Result:Retained considerable efficacy, with EC50 values of 1.5 and 1.6 × 10−6 M for HeLa and MRC5 cells, respectively.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb C nu/nu mice[2].
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Dosage:2 mg/kg in 0.3 mL solution via the lateral tail vein.
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Administration:IV.
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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.
Chemical Information
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CAS No. 490035-90-0
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Appearance Solid
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Molecular Weight 715.19
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Formula C34H24BBr2F2N3O2
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Color Brown to black
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SMILES
[F-][B+3]1([N]2=C(C3=CC=C(OC)C=C3)C(Br)=C(C4=CC=CC=C4)C2=NC5=C(C(Br)=C([N-]51)C6=CC=C(OC)C=C6)C7=CC=CC=C7)[F-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : < 1 mg/mL (insoluble or slightly soluble)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% Cremophor EL in PBS
Solubility: 2 mg/mL (2.80 mM); Suspended solution; Need ultrasonic
Purity & Documentation
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Data Sheet (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)