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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
Leukemic cells undergo dose-dependent apoptosis and cell cycle arrest in the G1 phase upon treatment with DCH36_06 (6.7–20 μM; 24-48 hours) [1]. The cleavage of pro-caspase 3, pro-caspase 9, and PARP1 is dramatically activated in a dose-dependent manner upon treatment with DCH36_06 (5-10 μM; 24 hours) [1]. When tested against the leukemia cell lines CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4;11, KOPN8, Kasumi-1, and K562 cells, DCH36_06 shown strong antiproliferative activity in a dose-dependent manner; its IC50 values are in the single-digit micromolar range [1].
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| ln Vivo |
DCH36_06 inhibits the growth of mouse leukemia xenografts when administered intraperitoneally (i.p.) at 25–50 mg/kg for 20 days [1].
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| Cell Assay |
Cell cycle analysis[1]
Cell Types: MV4-11 Cell Tested Concentrations: 6.7 μM, 20 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Dose-dependent cell cycle arrest in G1 phase. Apoptosis analysis [1] Cell Types: MV4-11 Cell Tested Concentrations: 6.7 μM, 20 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Significant induction of apoptosis. Western Blot Analysis [1] Cell Types: MV4-11 cells Tested Concentrations: 5 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Significant activation of pro-caspase 3, pro-caspase 9 and cleavage of PARP1 in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: MV4-11 xenograft nude mice [1]
Doses: 25 mg/kg, 50 mg/kg Route of Administration: intraperitoneal (ip) injection; every two days; 20 days Experimental Results: Tumor growth rate was Dramatically diminished in a dose-dependent manner . |
| References |
| Molecular Formula |
C18H13CLN2O3S
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|---|---|
| Molecular Weight |
372.825422048569
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| Exact Mass |
372.033
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| CAS # |
593273-05-3
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| PubChem CID |
1797299
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| Appearance |
Orange to red solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C)C=CC(=C1)N1C(NC(/C(=C\C=C\C2=CC=CO2)/C1=O)=O)=S
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| InChi Key |
AYNCXNUUERDREH-FMDPHQNASA-N
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| InChi Code |
InChI=1S/C18H13ClN2O3S/c1-11-7-8-12(10-15(11)19)21-17(23)14(16(22)20-18(21)25)6-2-4-13-5-3-9-24-13/h2-10H,1H3,(H,20,22,25)/b4-2+,14-6+
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| Chemical Name |
(5E)-1-(3-chloro-4-methylphenyl)-5-[(E)-3-(furan-2-yl)prop-2-enylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione
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| Synonyms |
DCH36-06; DCH36 06; DCH36_06
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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 : ~125 mg/mL (~335.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.58 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 (5.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6822 mL | 13.4109 mL | 26.8219 mL | |
| 5 mM | 0.5364 mL | 2.6822 mL | 5.3644 mL | |
| 10 mM | 0.2682 mL | 1.3411 mL | 2.6822 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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