| Size | Price | Stock | Qty |
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| 10mg |
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| ln Vitro |
DY-46-2 exhibits DNMT3A inhibitory activity with an IC50 value of 0.39 μM, increasing linearly with DNA concentration (IDT-01) [1]. It is available at concentrations ranging from 0.1 to 100 μM for 24, 48, and 72 hours. DY-46-2 (0.1-100 μM, 24, 48, and 72 h) exhibits inhibitory effect against G9a, DNMT1, and DNMT3B, with IC50 values of >500 μM, 105 μM, and 13.0 μM, respectively [1]. For HCT116, U937, K562, A549, DU145, and 72-hour exposure, DY-46-2 (0.1-100 μM, 24, 48, and 72 hours) had IC50 values of 0.7 μM, 0.3 μM, 0.7 μM, 0.5 μM, 2.1 μM, and 1.7 μM, and for THP 91 μM -1, respectively. Peripheral blood mononuclear cells (PBMCs) are not cytotoxic to DY-46-2 (0.1-100 μM, 24, 48, and 72 hours) and it effectively suppresses the proliferation of cancer cells [1]. In HCT116 cells, DY-46-2 (1 μM) dramatically lowers the reactive expression of silenced TSG (p53) and DNMT3A protein levels [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: THP-1, HCT116, U937, K562, A549, DU145 and PBMC Cell Tested Concentrations: 0.1-100 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Significant across the dose range Inhibited potency and time-dependent manner and was not cytotoxic in non-tumor PBMC (IC50 >100 μM). Cell proliferation assay[1] Cell Types: THP-1, HCT116, U937, K562, A549, DU145 and PBMC Cell Tested Concentrations: 0.1-100 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: demonstrated high anti-proliferative activity against All cancer cells have cytotoxicity in the micromolar range. Western Blot Analysis [1] Cell Types: HCT116 Cell Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: DNMT3A and p53 protein levels were diminished in HCT116 cells, apparently sufficient to reactively express silenced TSG (p53). |
| References |
| Molecular Formula |
C19H22N6O5S
|
|---|---|
| Molecular Weight |
446.480182170868
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| Exact Mass |
446.137
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| CAS # |
1105110-83-5
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| PubChem CID |
71035751
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| Appearance |
White to off-white solid powder
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
824
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1N(CCN2CCCC2)C(=O)C2C(C(NC3=CC=C(S(N)(=O)=O)N=C3)=O)=C(C)OC=2N=1
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| InChi Key |
FAZNWIGAOYXZGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N6O5S/c1-12-15(17(26)23-13-4-5-14(21-10-13)31(20,28)29)16-18(30-12)22-11-25(19(16)27)9-8-24-6-2-3-7-24/h4-5,10-11H,2-3,6-9H2,1H3,(H,23,26)(H2,20,28,29)
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| Chemical Name |
6-methyl-4-oxo-3-(2-pyrrolidin-1-ylethyl)-N-(6-sulfamoylpyridin-3-yl)furo[2,3-d]pyrimidine-5-carboxamide
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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 |
| 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 : ~50 mg/mL (~111.99 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2397 mL | 11.1987 mL | 22.3974 mL | |
| 5 mM | 0.4479 mL | 2.2397 mL | 4.4795 mL | |
| 10 mM | 0.2240 mL | 1.1199 mL | 2.2397 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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