Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
EB-3D is a novel potent and selective inhibitor of choline kinase αa1 (ChoKα1). EB-3D can induce the deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. EB-3D induces senescence in breast cancer cell lines through the activation of the metabolic sensor AMPK and the subsequent dephosphorylation of mTORC1 downstream targets, such as p70S6K, S6 ribosomal protein, and 4E-BP1. Moreover, EB-3D strongly synergizes with drugs commonly used for breast cancer treatment.
ln Vitro |
In both MEF and A549 cells, LRRK2-mediated phosphorylation of Rab10 and Rab12 is enhanced by L-leucyl-L-leucine methyl ester hydrobromide (1 mM; 0.5-2 h) [3]. CD4+ cells convert L-leucyl-L-leucine methyl ester hydrobromide (10-250 μM; 15 minutes) into an insoluble CCI3COOH compound [2].
|
---|---|
ln Vivo |
Mammary tumor growth is inhibited in a syngeneic orthotopic E0771-C57BL/6 mice model by EB-3D (1 mg/kg; ip; every other day)[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 cells Tested Concentrations: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI50s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively. Apoptosis Analysis[1] Cell Types: Jurkat, CCRF-CEM and HSB-2 cells Tested Concentrations: 1.25, 2.5, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis in leukemia cell lines. Cell Cycle Analysis[1] Cell Types: Jurkat, CCRF-CEM and HSB-2 cells Tested Concentrations: 0.5, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induces 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: demonstrated a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl- |
Animal Protocol |
Animal/Disease Models: E0771-C57BL/6 mice[4]
Doses: Ip; every other day for 4 weeks Route of Administration: 2.5 mg/kg Experimental Results: A reduction of the number of spontaneous lung macro- and micrometastasis. |
References |
|
Molecular Formula |
C30H36BR2N4O2
|
---|---|
Molecular Weight |
644.452
|
Elemental Analysis |
C, 55.91; H, 5.63; Br, 24.80; N, 8.69; O, 4.97
|
CAS # |
78218-09-4
|
Related CAS # |
74226-22-5 (HCl);78218-09-4;
|
Appearance |
Solid powder
|
SMILES |
CN(C1=CC=[N+](CC2=CC=C(OCCOC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2)C=C1)C.[Br-].[Br-]
|
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,21-24H2,1-4H32*1H/q+2/p-2
|
Synonyms |
EB-3D EB 3D EB3D
|
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) |
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 | 1.5517 mL | 7.7586 mL | 15.5171 mL | |
5 mM | 0.3103 mL | 1.5517 mL | 3.1034 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.