MLT-231
Based on 1 Customer Validation
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
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- Purity : 99.55%
- CAS No.: 2682102-10-7
- 화학식: C19H19ClF3N7O2
- 분자량:469.85
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BJAB | IC50 |
2 μM
Compound: 27; MLT-231
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Antiproliferation activity against human BJAB cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
Antiproliferation activity against human BJAB cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
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[PMID: 33252239] |
| BMDM | IC50 |
>10 μM
Compound: 27; MLT-231
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Cytotoxicity against mouse Bone marrow-derived macrophage cells assessed as reduction in cell viability by [3H]-thymidine incorporation assay
Cytotoxicity against mouse Bone marrow-derived macrophage cells assessed as reduction in cell viability by [3H]-thymidine incorporation assay
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[PMID: 33252239] |
| OCI-Ly3 | IC50 |
>10 μM
Compound: 27; MLT-231
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Antiproliferation activity against human OCI-LY3 cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
Antiproliferation activity against human OCI-LY3 cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
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[PMID: 33252239] |
| PBMC | IC50 |
0.19 μM
Compound: 27; MLT-231
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Inhibition of mixed lymphocyte reaction in human PBMC cells assessed as reduction in [3H]-thymidine incorporation measured after 5 days in presence of Il-7 by microbeta counting method
Inhibition of mixed lymphocyte reaction in human PBMC cells assessed as reduction in [3H]-thymidine incorporation measured after 5 days in presence of Il-7 by microbeta counting method
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[PMID: 33252239] |
In Vitro
MLT-231 (19.5-10000 nM) inhibits the proliferation of OCI-Ly3 cells. MLT-231 (50-5000 nM; 24 hours) leads to accumulation of the uncleaved form of its substrates CYLD, BCL10, and RELB while expression of the NF-κB target gene IRF4 is suppressed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:OCI-Ly3 cells
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Concentration:50-5000 nM
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Incubation Time:24 hours
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Result:NF-κB target gene IRF4 was suppressed.
In Vivo
MLT-231 (1 mg/kg; i.v.; BALB/c mice) treatment shows the CL, t1/2, and Vss are 11 mL/min/kg, 1.9 hours, and 1.5 L/kg, respectively[1].
MLT-231 (1 mg/kg; i.v.; Sprague-Dawley rats) treatment shows the CL, t1/2, and Vss are 41 mL/min/kg, 3.2 hours, and 9.4 L/kg, respectively[1].
MLT-231 (3 mg/kg; p.o.; BALB/c mice) treatment shows the AUC0-24, Cmax and F are 3096 nM/h, 549 nM, and 99%, respectively[1].
MLT-231 (3 mg/kg; p.o.; Sprague-Dawley rats) treatment shows the AUC0-24, Cmax and F are 547 nM/h, 46 nM, and 61%, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)[1]
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Dosage:10, 30, and 100 mg/kg
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Administration:P.o.; bid schedule for 2 weeks
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Result:Led to tumor stasis, while being well tolerated.
Chemical Information
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CAS No. 2682102-10-7
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Appearance Solid
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분자량 469.85
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화학식 C19H19ClF3N7O2
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Color White to off-white
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SMILES
O=C(NC1=C(N2[C@@H](C)COC[C@@H]2C)N3C(N=C1)=CC(Cl)=N3)NC4=CC=NC(C(F)(F)F)=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 110 mg/mL (234.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6 mg/mL (12.77 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
순도&문서
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1283 mL | 10.6417 mL | 21.2834 mL | 53.2085 mL |
| 5 mM | 0.4257 mL | 2.1283 mL | 4.2567 mL | 10.6417 mL | |
| 10 mM | 0.2128 mL | 1.0642 mL | 2.1283 mL | 5.3208 mL | |
| 15 mM | 0.1419 mL | 0.7094 mL | 1.4189 mL | 3.5472 mL | |
| 20 mM | 0.1064 mL | 0.5321 mL | 1.0642 mL | 2.6604 mL | |
| 25 mM | 0.0851 mL | 0.4257 mL | 0.8513 mL | 2.1283 mL | |
| 30 mM | 0.0709 mL | 0.3547 mL | 0.7094 mL | 1.7736 mL | |
| 40 mM | 0.0532 mL | 0.2660 mL | 0.5321 mL | 1.3302 mL | |
| 50 mM | 0.0426 mL | 0.2128 mL | 0.4257 mL | 1.0642 mL | |
| 60 mM | 0.0355 mL | 0.1774 mL | 0.3547 mL | 0.8868 mL | |
| 80 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6651 mL | |
| 100 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5321 mL |
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