| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
STAT3
|
|---|---|
| ln Vitro |
HJC0416 hydrochloride, with IC50 values of 1.76 µM and 1.97 µM, respectively, inhibits the proliferation of both ER-positive and ER-negative (triple negative) breast cancer cells. AsPC1 and Panc-1, two pancreatic cancer cell lines, exhibit a strong antiproliferative impact against it, with IC50 values of 40 nM and 1.88 µM, respectively[1]. HJC0416 hydrochloride (1–10 µM; 48 hours) causes apoptosis and suppresses cell proliferation in MDA-MB-231 breast cancer cells, along with alterations in cellular morphology[1].The STAT3 promoter activity is reduced by about 51% in MDA-MB-231 cells transiently transfecting with the pSTAT3-Luc vector, but stattic (HY-13818) only reduces the STAT3 promoter activity by 39%[1]. Comparing HJC0416 hydrochloride (1–10 µM; 12 hours) to Stattic (HY-13818), it is equally effective in inhibiting the synthesis of STAT3 proteins and phosphorylation at the Tyr-705 site. In MDA-MB-231 cells, it also causes cleaved caspase-3 and downregulates cyclin D1 levels[1].
|
| ln Vivo |
In comparison to the control mice, the intraperitoneal injection of HJC0416 hydrochloride (10 mg/kg) results in a 67% reduction in tumor volume after 7 days. Likewise, at a dose of 100 mg/kg, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) likewise significantly lowers tumor volume by 46%. Tumor volume decrease seemed to be superior with the ip approach. It is particularly remarkable that, at a dose of 100 mg/kg, HJC0416 does not exhibit any discernible toxicity[1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: MDA- MB-231 breast cancer cells Tested Concentrations: 1-10 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell apoptosis in cancer cells. Apoptosis Analysis[1] Cell Types: MDA-MB-231 breast cancer cells Tested Concentrations: 1 µM; 5 µM; 10 µM Incubation Duration: 12 hrs (hours) Experimental Results: diminished p-STAT3 phosphorylation expression and cyclin D1 level. |
| Animal Protocol |
Animal/Disease Models: Mice with MDA-MB-231 cells[1]
Doses: 10 mg/kg (ip); 100 mg/kg (oral) Route of Administration: intraperitoneal (ip)injection, 7 days; oral administration, 14 days Experimental Results: demonstrated antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model. |
| References |
[1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.
|
| Molecular Formula |
C18H18CL2N2O4S
|
|---|---|
| Molecular Weight |
429.32
|
| CAS # |
2415263-08-8
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=S1(C=CC2=CC=C(NC(C3C=C(Cl)C=CC=3OCCCN)=O)C=C12)=O.Cl
|
| 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 | 2.3293 mL | 11.6463 mL | 23.2926 mL | |
| 5 mM | 0.4659 mL | 2.3293 mL | 4.6585 mL | |
| 10 mM | 0.2329 mL | 1.1646 mL | 2.3293 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
