| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
HDAC1 19.75 nM (IC50) HDAC6 5.63 nM (IC50) HDAC3 40.27 nM (IC50) HDAC2 57.8 nM (IC50) HDAC8 302.73 nM (IC50)
|
|---|---|
| ln Vitro |
Compound 21, or HDAC-IN-47, has an IC50 value of 0.24 μM and suppresses the development of A549 cells with antiproliferative activity[1]. In A549 cells, HDAC-IN-47 (0.5 and 1 μM; 72 h) causes apoptosis and shows a deep G2/M arrest[1]. Bax and Caspase 3 expression levels are raised, Bcl-2 levels are lowered, and the intrinsic (mitochondrial) apoptotic pathway is activated by HDAC-IN-47 (0.1 and 0.5 μM; 24 h)[1].
|
| ln Vivo |
Compound 21, or HDAC-IN-47, (50 and 100 mg/kg; po; once daily; 18 d) in the A549 xenograft mice model shows considerable anticancer efficacy in a dose-dependent manner without causing any appreciable body weight loss[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HepG2, MDA-MB-238, HL-60 cells Tested Concentrations: 0.16-0.45 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cancer cells with IC50s of 0.16 μM(HepG2), 0.45 μM (MDA-MB-238), 0.22 μM(HL-60), respectively. Cell Cycle Analysis[1] Cell Types: A549 cells Tested Concentrations: 0.5 and 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced marked arrest of cells in the G2 /M phase of 28.38%(0.5 μM) and 31.70%(1.0 μM). Apoptosis Analysis[1] Cell Types: A549 cells Tested Concentrations: 0.5 and 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Resulted 21.09%(0.5 μM) and 30.58 %(1 μM) apoptotic cells. |
| Animal Protocol |
Animal/Disease Models: A549 xenograft model in mouse (female, BALB/c nu/nu (nude) mice, 6-8 weeks old)[1]
Doses: 50 mg/kg; 100 mg/kg Route of Administration: po (oral gavage); one time/day; for 18 days Experimental Results: diminished the tumor volume and weight by 48% and 45%, respectively. |
| References |
| Molecular Formula |
C17H20BRN3O4
|
|---|---|
| Molecular Weight |
410.26
|
| Appearance |
Typically exists as solid at room temperature
|
| 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 | 2.4375 mL | 12.1874 mL | 24.3748 mL | |
| 5 mM | 0.4875 mL | 2.4375 mL | 4.8750 mL | |
| 10 mM | 0.2437 mL | 1.2187 mL | 2.4375 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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