| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
DNMT-IN-5 (compound 34b) (0.1–30 μM; 3 days) still exhibited DNMT 3A inhibitor activity at nanomolar concentrations, with an IC50 value of 9.15 μM in HCT-116 cells[1]. DNMT-IN-5 (5 μM; 0–5 days) significantly upregulated the expression of p15 and p16 in HCT-116 cells, upregulating them by 1.76-fold (88%) and 1.34-fold (67%), respectively[1]. The effect of DNMT-IN-5 (5 μM; 5 days) on DNMT-regulated genes varied by cell type, with the most significant effect observed in HCT-116 cells[1]. DNMT-IN-5 (5 μM; 5 days) induced a critical arrest of the cell cycle in the G1/S phase, particularly in p53-deficient HCT-116 colorectal cancer cells[1].
|
|---|---|
| Cell Assay |
Cell viability assay [1]
Cell Types: HCT-116 Tested Concentrations: 0.1 μM; 1 μM; 10 μM; 100 μM Incubation Duration: 3 days Experimental Results: Very similar cytotoxicity was observed between each other and with reference compound MLo1506 (IC50 = 8.18 μM) (IC50 = 9.15 μM). RT-PCR[1] Cell Types: HCT-116 Tested Concentrations: 5 μM Incubation Duration: 0 days; 2 days; 5 days Experimental Results: Compared with untreated cells, p15 expression was significantly upregulated by 1.76-fold (88%). p16 expression increased by 1.34-fold (67%). Cell cycle analysis [1] Cell Types: HCT-116, DU-145, U2OS Tested Concentrations: 5 μM Incubation Duration: 5 days Experimental Results: The expression of p15 in p53 knockout cells was not altered, but the re-expression of p16 was successfully induced. In the absence of p53, the G1/S phase transition was significantly inhibited, leading to the emergence of a large number of replication-deficient cells. |
| References |
| Molecular Formula |
C16H12BRCLO3
|
|---|---|
| Molecular Weight |
367.62
|
| CAS # |
3126555-64-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CO[C@]1(C2=CC=CC=C2)OC3=CC=CC=C3C([C@@]1(Cl)Br)=O
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.7202 mL | 13.6010 mL | 27.2020 mL | |
| 5 mM | 0.5440 mL | 2.7202 mL | 5.4404 mL | |
| 10 mM | 0.2720 mL | 1.3601 mL | 2.7202 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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