| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
With GI GI50s 13 values in the nanomolar range, EB-3D has outstanding antiproliferative action against several T leukemia cell lines (0-100 μM; 72 hours) [1]. In leukemia cell lines, EB-3D (1.25-5μM; 24 hours) causes apoptosis [1]. G0/G1 arrest is induced by EB-3D (0.5-1 μM; 24 hours), which results cell apoptosis [1]. After 30 minutes, AMPKα is first activated in EB-3D (0.3 μM; 48 hours), which is followed by enhanced T172 phosphorylation [1]. HepG2 cell proliferation is inhibited by EB-3D (1-40 μM; 48 hours) with a GI50 of 14.55 μM [2]. In leukemic T cells, EB-3D causes deregulation of the AMPK-mTOR pathway and apoptosis [1].
|
|---|---|
| ln Vivo |
In the syngeneic orthotopic E0771-C57BL/6 mouse model, EB-3D (1 mg/kg; i.p.; every other day) inhibits the formation of breast tumors [4]. For four weeks, EB-3D (2.5 mg/kg; every other day) reduced the amount of spontaneous lung macro- and micrometastases [4].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL Cell Tested Concentrations: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER and ALL-SIL cell growth with GI50 of 136.2, 478.8, 17.7, 0.9, 60.6, 200, respectively are 265 and 132 nM. Apoptosis analysis [1] Cell Types: Jurkat, CCRF-CEM and HSB-2 Cell Tested Concentrations: 1.25, 2.5, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis in leukemia cell lines. Cell cycle analysis [1] Cell Types: Jurkat, CCRF-CEM and HSB-2 Cell Tested Concentrations: 0.5, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced cell cycle arrest in G0/G1 phase. Western Blot Analysis [1] Cell Types: Jurkat cells Tested Concentrations: 0.3 μM Incubation Duration: 48 hrs (hours) Experimental Results: The first activation peak of AMPKα occurred after 30 minutes of treatment, followed by an increase in T172 phosphorylation. The same pattern was followed by increased S79 phosph |
| Animal Protocol |
Animal/Disease Models: E0771-C57BL/6 mice [4]
Doses: Ip; every other day for 4 weeks: 2.5 mg/kg Experimental Results: The number of spontaneous lung macro and micro metastases was diminished. |
| References |
|
| Molecular Formula |
C₃₀H₃₆BR₂N₄O₂MOLECULARWEIGHT
|
|---|---|
| Molecular Weight |
644.44
|
| Exact Mass |
644.118
|
| Elemental Analysis |
C, 55.91; H, 5.63; Br, 24.80; N, 8.69; O, 4.97
|
| CAS # |
1839150-63-8
|
| Related CAS # |
1839150-62-7 (cation);1839150-63-8 (bromide);
|
| PubChem CID |
90467110
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
38
|
| Complexity |
534
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SCXVGPSPZQBBDM-UHFFFAOYSA-L
|
| InChi Code |
InChI=1S/C30H36N4O2.2BrH/c1-31(2)27-13-17-33(18-14-27)23-25-5-9-29(10-6-25)35-21-22-36-30-11-7-26(8-12-30)24-34-19-15-28(16-20-34)32(3)4;;/h5-20H,21-24H2,1-4H3;2*1H/q+2;;/p-2
|
| Chemical Name |
1-[[4-[2-[4-[[4-(dimethylamino)pyridin-1-ium-1-yl]methyl]phenoxy]ethoxy]phenyl]methyl]-N,N-dimethylpyridin-1-ium-4-amine;dibromide
|
| Synonyms |
EB3D; EB 3D
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~50 mg/mL (~77.59 mM)
H2O : ≥ 9.09 mg/mL (~14.11 mM) |
|---|---|
| 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 | 1.5517 mL | 7.7587 mL | 15.5173 mL | |
| 5 mM | 0.3103 mL | 1.5517 mL | 3.1035 mL | |
| 10 mM | 0.1552 mL | 0.7759 mL | 1.5517 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
