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Purity: ≥98%
MI-2 (also known as MALT1 inhibitor) is a potent and irreversible MALT1 inhibitor with IC50 of 5.84 μM, and binds directly to MALT1, irreversibly suppresses protease function. MI-2 inhibits MALT1 functions in ABC-DLBCL cell lines with excellent cell penetration. MI-2 binds directly to MALT1 and irreversibly suppresses protease function. Decreases NF-κB activity induced by MALT1. MI-2 produces selective growth inhibition for MALT1-dependent cell lines with GI50 of 0.2, 0.5, 0.4, and 0.4 μM in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, whereas the ABC-DLBCL MALT1-independent cell lines, U2932 and HLY-1, and the two GCB-DLBCL cell lines were resistant.
| ln Vitro |
MALT1-dependent DLBCL cell lines are selectively suppressed by the MALT1 inhibitor MI-2 (1-1000 nM; 48 hours); the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 μM, respectively[1]. MALT1-mediated cleavage is reduced in a dose-dependent manner by the MALT1 inhibitor MI-2 (62-1000 nM; 24 hours)[1]. MALT1 blocker
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| ln Vivo |
The growth of TMD8 and HBL-1 ABC-DLBCL xenografts is significantly suppressed by the MALT1 inhibitor MI-2 (25 mg/kg; ip; daily for 14 days)[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HBL -1, TMD8, OCI-Ly3, OCI-Ly10 cells Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 48 hrs (hours) Experimental Results: The GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 µM, respectively. Western Blot Analysis[1] Cell Types: HBL-1 cells Tested Concentrations: 62, 125, 250, 500, 1000 nM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibits MALT1 cleavage of CYLD in HBL -1 cells. |
| Animal Protocol |
Animal/Disease Models: Eightweeks old male SCID NOD ( bearing HBL-1 and TMD8 cells)[1]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip)injection; daily for 14 days Experimental Results: Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle. |
| References |
[1]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.
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| Molecular Formula |
C19H17CL3N4O3
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| Molecular Weight |
455.72
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| CAS # |
1047953-91-2
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| Related CAS # |
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(NC1=CC=C(N2N=C(OCCOC)N=C2C3=CC=C(Cl)C(Cl)=C3)C=C1)CCl
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.49 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 (5.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: 2% DMSO +30%PEG 300: 5 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1943 mL | 10.9716 mL | 21.9433 mL | |
| 5 mM | 0.4389 mL | 2.1943 mL | 4.3887 mL | |
| 10 mM | 0.2194 mL | 1.0972 mL | 2.1943 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04876092 | ACTIVE,NOT RECRUITING | Drug:JNJ-67856633 Drug:Ibrutinib |
Leukemia,Lymphocytic, Chronic,B-Cell Lymphoma, Non-Hodgkin |
Janssen Research & Development, LLC |
2021-07-28 | Phase 1 |
| NCT05618028 | RECRUITING | Drug:ABBV-525 | B Cell Malignancies Chronic Lymphocytic Leukemia Diffuse Large B-Cell Lymphoma Non-Hodgkin's Lymphoma |
AbbVie | 2023-04-04 | Phase 1 |
| NCT03900598 | ACTIVE,NOT RECRUITING | Drug:JNJ-67856633 | Leukemia,Lymphocytic, Chronic,B-Cell Lymphoma, Non-Hodgkin |
Janssen Research&Development,LLC | 2019-04-03 | Phase 1 |
| NCT05544019 | RECRUITING | Drug:SGR-1505 | ALK-Positive Large B-Cell Lymphoma Burkitt Lymphoma Chronic Lymphocytic Leukemia DLBCL |
Schrödinger,Inc. | 2023-04-10 | Phase 1 |
| NCT04882475 | RECRUITING | Mantle Cell Lymphoma | Fondazione Italiana Linfomi-ETS | 2023-02-08 |
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