| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IC50: 5 nM (MALT1)[1] Kd: 13 nM (MALT1(329-728)-W580S), 42 nM (MALT1(329-728))[1]
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|---|---|
| ln Vitro |
With the same affinity as wild-type MALT1 (329-728) (Kd, 42 nM), MLT-748 reversibly binds the human mutant MALT1 (329-728)-W580S (Kd, 13 nM) [1]. MALT1-W580S cells, EC50 69 nM, are stabilized by MLT-748 (0-2 μM)[1]. MLT-748 (2 μM, 24 hours) phosphorylates IκBα and p65 in immortalized B cells from MALT1mut/mut patients [1].
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| Cell Assay |
Western Blot Analysis
Cell Types: MALT1mut/mut patient immortalized B cells Tested Concentrations: 2 µM Incubation Duration: 24 hrs (hours) Experimental Results: Increased NF-κB signaling phosphorylation of both p65 and IκBα as early as 5 min after stimulation with PMA and ionomycin. |
| References |
[1]. Quancard J, et al. An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient. Nat Chem Biol. 2019 Mar;15(3):304-313.
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| Molecular Formula |
C19H19CL2N9O3
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|---|---|
| Molecular Weight |
492.32
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| CAS # |
1832578-30-9
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| SMILES |
ClC1C=C2N=CC(=C([C@H]([C@@H](C)OC)OC)N2N=1)NC(NC1C=NC(=C(C=1)Cl)N1N=CC=N1)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Solubility (In Vitro) |
DMSO: 200 mg/mL (406.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.22 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.22 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. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.22 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0312 mL | 10.1560 mL | 20.3120 mL | |
| 5 mM | 0.4062 mL | 2.0312 mL | 4.0624 mL | |
| 10 mM | 0.2031 mL | 1.0156 mL | 2.0312 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.
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