| Targets |
LM-41 targets TEAD (TEA domain) transcription factors, with particular affinity for TEAD4. It is a covalent inhibitor of TEAD4. Inhibition of TEAD disrupts the Hippo signaling pathway, which plays a critical role in organ size control, tissue homeostasis, and tumorigenesis. LM-41 strongly reduces the expression of TEAD target genes including CTGF, Cyr61, Axl, and NF2.
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| ln Vitro |
In vitro, LM-41 functions as a TEAD inhibitor. It strongly reduces the expression of TEAD target genes CTGF, Cyr61, Axl, and NF2. At a concentration of 10 µM, LM-41 significantly inhibits the migration of human MDA-MB-231 breast cancer cells. It is also noted to have potential anticancer activity.
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| ln Vivo |
Specific in vivo activity data for LM-41 are not detailed in the available literature. However, its potent in vitro activity as a TEAD inhibitor and its ability to inhibit breast cancer cell migration suggest potential for in vivo efficacy in cancer models. As a TEAD inhibitor, it may have applications in studying Hippo pathway-related cancers.
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| Enzyme Assay |
Non-cellular binding assays for LM-41 would typically involve measuring its binding affinity to TEAD4. These assays can be performed using techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) with purified TEAD4 protein. As a covalent inhibitor, its binding kinetics and mechanism of action can be characterized in detail.
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| Cell Assay |
In vitro cellular assays for LM-41 are performed using cancer cell lines, particularly human MDA-MB-231 breast cancer cells. Cells are treated with LM-41, and the expression of TEAD target genes (CTGF, Cyr61, Axl, and NF2) is measured by qRT-PCR or Western blotting. Cell migration is assessed using wound healing or transwell migration assays at concentrations such as 10 µM.
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| Animal Protocol |
In vivo animal experiments for LM-41 would typically be conducted in mouse models of cancer, such as breast cancer xenografts. The compound would be administered via intraperitoneal or oral routes, and endpoints would include tumor growth inhibition, assessment of TEAD target gene expression in tumors, and evaluation of metastasis.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for LM-41 are not detailed in the available sources. The compound has a molecular weight of 307.32 and a molecular formula of C19H14FNO2. It is soluble in DMSO (140 mg/mL) and should be stored at 4°C, protected from light, and under nitrogen.
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| Toxicity/Toxicokinetics |
Toxicological data for LM-41 are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized. It is intended for research use only and not for human or veterinary use.
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| References | |
| Additional Infomation |
LM-41 has a molecular formula of C19H14FNO2 and a molecular weight of 307.32. Its CAS number is 2996821-30-6. The formal name is 2-([1,1'-biphenyl]-3-ylamino)-5-fluorobenzoic acid. LM-41 is a covalent TEAD4 inhibitor that reduces migration of breast cancer cells. It is a valuable tool for studying Hippo pathway signaling and TEAD function in cancer biology. It is not approved for clinical use.
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| CAS # |
2996821-30-6
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| Appearance |
White to off-white solid powder
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| Density |
1.293±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
479.4±45.0 °C(predicted)
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| LogP |
0
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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 |
| 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) |
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
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| 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.) |
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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