| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Protein arginine methyltransferase 1 (PRMT1). DCLX069 is a selective PRMT1 inhibitor that occupies the SAM binding pocket to exert its inhibitory effect. PRMT1 is the predominant type I protein arginine methyltransferase responsible for the majority of cellular asymmetric dimethylarginine (ADMA) production and plays important roles in transcriptional regulation, DNA damage repair, and signal transduction.
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| ln Vitro |
In a concentrated cell form, DCLX069 (12.5-100 μM) efficiently inhibits cell growth in acute leukemia, bone marrow, and breast cancer cell lines (MCF7, HepG2, and THP1) [1].
DCLX069 effectively blocks cell proliferation in breast cancer, liver cancer, and acute myeloid leukemia cell lines. The compound demonstrates anticancer activity with an IC50 of 17.9 μM against PRMT1. It shows low activity against PRMT4 and PRMT6, indicating selectivity for PRMT1 over other PRMT family members. |
| ln Vivo |
DCLX069 has reported anticancer activity. In vivo efficacy studies suggest that PRMT1 inhibition by DCLX069 may have therapeutic potential in various cancer types. However, detailed in vivo pharmacokinetic and efficacy data are limited, and further studies are needed to fully characterize the compound's in vivo activity and therapeutic window.
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| Enzyme Assay |
In vitro enzyme inhibition assays for DCLX069 typically use purified recombinant PRMT1 enzyme and a suitable substrate such as histone H4 or a peptide substrate. The assay measures the transfer of 3H-methyl groups from S-adenosyl-[3H]methionine (SAM) to the substrate. DCLX069 is incubated with the enzyme, substrate, and radiolabeled SAM at varying concentrations, and the methyltransferase activity is quantified by measuring incorporated radioactivity. IC50 values are calculated from dose-response curves.
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| Cell Assay |
DCLX069 is tested in various cancer cell lines including breast cancer (e.g., MCF-7, MDA-MB-231), liver cancer (e.g., HepG2), and acute myeloid leukemia (e.g., HL-60, MV4-11) cell lines. Cells are treated with DCLX069 at concentrations ranging from 0 to 100 μM for 48-72 hours. Cell proliferation is assessed using MTT, CCK-8, or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining or caspase-3/7 activity assays. PRMT1 inhibition and subsequent changes in protein arginine methylation are confirmed by Western blot using specific anti-methylarginine antibodies.
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| Animal Protocol |
In vivo studies for DCLX069 are typically performed in mouse xenograft models using cancer cell lines that are sensitive to PRMT1 inhibition. Tumor-bearing mice are administered DCLX069 via intraperitoneal or oral routes at various doses. Tumor volume is monitored every 2-3 days using calipers. At study termination, tumors are excised and analyzed for PRMT1 inhibition, changes in protein arginine methylation, and markers of apoptosis and proliferation. Body weight and overall health are monitored throughout the study to assess tolerability.
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| ADME/Pharmacokinetics |
DCLX069 has a molecular weight of 339.43 and molecular formula C20H25N3O2. It is soluble in DMSO (60 mg/mL, 176.77 mM) and should be stored as powder at -20°C for 3 years or in solvent at -80°C for 1 year. For in vivo formulation, a recommended vehicle is 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline (2 mg/mL, 5.89 mM).
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| Toxicity/Toxicokinetics |
Available toxicology data for DCLX069 are limited to in vitro cell-based assays. At effective concentrations, the compound inhibits cancer cell proliferation. Standard safety precautions should be followed when handling DCLX069, as with all small-molecule inhibitors. No specific acute or chronic toxicity data have been reported in the literature. The compound is for research use only and is not for human therapeutic use.
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| References | |
| Additional Infomation |
DCLX069 is a research-use only compound and has not yet entered clinical trials. It is a novel, SAM-competitive, and selective PRMT1 inhibitor with anticancer effects. The compound is used as a tool to study the role of PRMT1-mediated protein arginine methylation in cancer biology and to validate PRMT1 as a therapeutic target. DCLX069 has shown efficacy in blocking proliferation in breast cancer, liver cancer, and acute myeloid leukemia cell lines.
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| Molecular Formula |
C20H25N3O2
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|---|---|
| Molecular Weight |
339.439
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| Exact Mass |
339.194
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| CAS # |
792946-69-1
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| PubChem CID |
2997002
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
515.9±50.0 °C at 760 mmHg
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| Flash Point |
265.8±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.611
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| LogP |
2.63
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
417
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=CC(=C(C=C1)N2CCN(CC2)CC3=CC=CC=C3)N
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| InChi Key |
RITRCMIWRZBDID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N3O2/c1-2-25-20(24)17-8-9-19(18(21)14-17)23-12-10-22(11-13-23)15-16-6-4-3-5-7-16/h3-9,14H,2,10-13,15,21H2,1H3
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| Chemical Name |
ethyl 3-amino-4-(4-benzylpiperazin-1-yl)benzoate
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| Synonyms |
DCLX 069 DCLX-069 DCLX069
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~294.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 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 25.0 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: ≥ 2.5 mg/mL (7.37 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 25.0 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: ≥ 2.5 mg/mL (7.37 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 | 2.9460 mL | 14.7301 mL | 29.4603 mL | |
| 5 mM | 0.5892 mL | 2.9460 mL | 5.8921 mL | |
| 10 mM | 0.2946 mL | 1.4730 mL | 2.9460 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.
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