| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
| Targets |
MALT1[1]
|
|---|---|
| ln Vitro |
In activated B-cell subtypes of diffuse large B-cell lymphoma (ABCDLBCL) cells, mepazine (5–20 μM; 4 days) reduces cell survival; however, it has no discernible effect on GCB-DLBCL cells [1].
|
| ln Vivo |
Mepazine (16 mg/kg; i.p.) inhibits the development of the ABC-DLBCL cell line OCI-Ly10 in NOD/scid IL-2RgnuLl (NSG) mice and causes apoptosis. Mepazine given daily significantly inhibits the ABC-DLBCL cell line OCI-Ly10's ability to proliferate [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: ABC-DLBCL cell lines (HBL1, OCI-Ly3, U2932, TMD8, OCI-Ly10 ) and GCB-DLBCL cell lines (BJAB, Su-DHL-6, Su-DHL-4) Tested Concentrations: 5, 10, and 20 μM Incubation Duration: 4 days Experimental Results: Caused a decrease of cell viability in the ABC-DLBCL cells HBL1, OCI-Ly3, U2932, and TMD8, without Dramatically affecting GCB-DLBCL cells. |
| Animal Protocol |
Animal/Disease Models: 6- to 8weeks old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with a murine DLBCL xenogeneic tumor model[1]
Doses: 400 μg per animal (25 g), corresponding to approximately 16 mg/kg Route of Administration: intraperitoneal (ip)administration; started 1 or 12 days after transplantation and given continuously every 24 hr; daily application Experimental Results: Daily administration strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10. |
| References |
[1]. Nagel D, et al. Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL. Cancer Cell. 2012 Dec 11;22(6):825-37.
|
| Molecular Formula |
C19H23CLN2S
|
|---|---|
| Molecular Weight |
346.92
|
| CAS # |
2975-36-2
|
| Related CAS # |
Mepazine;60-89-9
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
Cl.CN1CCCC(CN2C3=CC=CC=C3SC3=CC=CC=C23)C1
|
| 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 (144.13 mM)
H2O : 2.22 mg/mL (6.40 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1.25 mg/mL (3.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8825 mL | 14.4125 mL | 28.8251 mL | |
| 5 mM | 0.5765 mL | 2.8825 mL | 5.7650 mL | |
| 10 mM | 0.2883 mL | 1.4413 mL | 2.8825 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
