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5mg |
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25mg |
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Purity: ≥98%
DIM-C-pPhOH (also known as C-DIM8) is a Nur77 (NR4A1) antagonist. In a metastasis model, DIM-C-pPhOH prevents the growth of lung cancer cells and tumors. When pancreatic and colon cancer cells are treated with C-DIM8, it mimics the effects of NR4A1 knockdown and lowers the expression of β1-integrin, as well as β1-integrin-regulated genes and responses, such as migration and adhesion. A member of the nuclear receptor family of transcription factors' nerve growth factor-I-B subfamily, Nur77 is an orphan receptor. The findings show a fresh approach for β1-integrin targeting in pancreatic and colon cancer cells and suggest potential clinical uses for C-DIM/NR4A1 antagonists in the treatment of colon and pancreatic cancer.
Targets |
Nur77 (IC50 = 13.0 μM); Nur77 (IC50 = 13.6 μM)
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ln Vitro |
DIM-C-pPhOH (7.5-20 μM; 24 hours; ACHN and 786-O cells) treatment significantly decreases cell proliferation[1].
DIM-C-pPhOH (20 μM; 24 hours; ACHN and 786-O cells) treatment results in Annexin V staining in ACHN and 786-O cells, confirming that DIM-C-pPhOH induces apoptosis and also induces caspase 7 and 8 cleavage[1]. DIM-C-pPhOH (15-20 μM; 24 hours; ACHN and 786-O cells) treatment inhibits NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-O cells. Additionally, it activates AMPK, stimulates sestrin 2, and inhibits the activation of mTOR and downstream kinases[1]. DIM-C-pPhOH reduces expression of β1-integrin protein and mRNA as well as β1-integrin-dependent responses in MCF7, MDA-MB-231, and SKBR3. The latter two cell lines are also prevented from migrating[2]. |
ln Vivo |
DIM-C-pPhOH (30 mg/kg; oral gavage; daily; for 50 days; male athymic nude mice) treatment results in a significant inhibition of tumor growth[1].
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References |
Molecular Formula |
C23H18N2O
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Molecular Weight |
338.41
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Exact Mass |
338.14
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Elemental Analysis |
C, 81.63; H, 5.36; N, 8.28; O, 4.73
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CAS # |
151358-47-3
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C1=CC=C2C(=C1)C(=CN2)C(C3=CC=C(C=C3)O)C4=CNC5=CC=CC=C54
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InChi Key |
QCPDFNWJBQMXLI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H18N2O/c26-16-11-9-15(10-12-16)23(19-13-24-21-7-3-1-5-17(19)21)20-14-25-22-8-4-2-6-18(20)22/h1-14,23-26H
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Chemical Name |
4-[bis(1H-indol-3-yl)methyl]phenol
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 68~125 mg/mL(201.0~369.4 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9550 mL | 14.7750 mL | 29.5500 mL | |
5 mM | 0.5910 mL | 2.9550 mL | 5.9100 mL | |
10 mM | 0.2955 mL | 1.4775 mL | 2.9550 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NR4A1 regulates β1-integrin and β1-integrin-regulated genes/gene activation.Mol Carcinog.2017 Sep;56(9):2066-2075. th> |
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NR4A1 regulates pancreatic and colon cancer cell migration.Mol Carcinog.2017 Sep;56(9):2066-2075. td> |
β1-Integrin-dependent migration is dependent on NR4A1.Mol Carcinog.2017 Sep;56(9):2066-2075. td> |