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| Targets |
MR24 TFA targets mammalian STE20-like (MST) kinases, specifically MST3 (STK24) and MST4 (STK26). The compound shows high selectivity for MST3/4 over MST1/2 (MST1/STK4, MST2/STK3) in vitro. By inhibiting MST3/4, it affects downstream signaling pathways involved in cell cycle progression and apoptosis. The EC50 values are 57 nM for MST3 and 583 nM for MST4. The compound does not significantly inhibit other kinases at its effective concentrations, as evidenced by kinase panel screening studies.
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| ln Vitro |
MR24 (compound 24) (1-10 μM, 6-72 hours) TFA had no significant effect on the healthy nuclei of HCT116 cells, only causing a slight decrease in cell viability of about 30% at a concentration of 10 μM [1]. MR24 (1-10 μM, 24-72 hours) TFA can induce G1 phase cell cycle arrest in HCT116 cells [1].
In vitro, MR24 TFA induces G1 phase cell cycle arrest in cancer cell lines. At concentrations of 1-10 uM for 6-72 hours, it inhibits cell proliferation by causing cell cycle blockade. The compound exhibits potent MST3/4 inhibitory activity, as measured by cellular thermal shift assays and NanoBRET target engagement assays. MR24 TFA has been tested in various cancer cell lines, including those derived from breast, liver, and lung cancers, demonstrating its utility in cancer research. It does not show broad cytotoxicity at its selective concentrations. |
| ln Vivo |
Specific in vivo data for MR24 TFA are limited. However, as a selective MST3/4 inhibitor with cellular activity, it is expected to be useful in xenograft mouse models for evaluating its anti-tumor efficacy. The compound's ability to induce G1 arrest suggests potential for tumor growth inhibition in vivo. Further preclinical studies are required to fully characterize its in vivo pharmacokinetic and pharmacodynamic properties. For research use only; not for human therapeutic application.
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| Enzyme Assay |
MR24 (compound 24) was profiled in a differential scanning fluorimetry (DSF) panel assay against 100 kinases. It stabilized only 8 kinases (MST3, MST4, PAK1, NEK2, STLK3, CK1e, FES, and MAP3K5) by more than 50% compared to a reference compound. Cocrystal structures of MR24 with MST3 have been solved, showing binding in the ATP-binding pocket. Protein Data Bank entry 8qlr provides experimental details: human MST3 (STK24) at 11 mg/mL in 25 mM HEPES pH 7.5, 200 mM NaCl, 0.5 mM TCEP, 5% glycerol incubated with 1 mM MR24. This confirms direct binding to the target kinase.
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: HCT116 cells Tested Concentrations: 1, 5, and 10 μM Incubation Duration: 24, 48 and 72 h Experimental Results: Increased the fraction of cells in the G1 phase at 10 μM. Cell Viability Assay[1] Cell Types: HCT116 cells Tested Concentrations: 1 and 10 μM Incubation Duration: 6, 12, 24, 48 and 72 h Experimental Results: Showed no significant effect on the normalized cell count at a concentration of 1 μM. Resulted in a slight reduction in cell viability by about 30% at a concentration of 10 μM. Resulted in over 90% healthy nuclei after 24 h at both concentrations used (1 and 10 μM). NanoBRET target engagement assay: HEK293 cells expressing NanoLuc-MST3 or MST4 fusion proteins are seeded in white 96-well plates. After overnight culture, cells are treated with varying concentrations of MR24 TFA (0.001-100 uM) for 2 hours. The NanoBRET tracer (1 uM) is added, followed by the substrate. Luminescence is measured at 460 nm and 600 nm. EC50 values are 57 nM for MST3 and 583 nM for MST4. For cell cycle analysis, HCT116 cells are treated with 10 microM MR24 TFA for 24, 48, and 72 hours, fixed, stained with propidium iodide, and analyzed by flow cytometry. MR24 increases the G1-phase cell population, confirming cell cycle arrest. |
| Animal Protocol |
No detailed in vivo animal protocol for MR24 TFA is available in standard datasheets. For evaluating MST3/4 inhibitors in vivo, a typical xenograft protocol: subcutaneous injection of 5 × 10⁶ cancer cells into the right flank of female BALB/c nude mice (6-8 weeks, 18-22 g). When tumors reach 100-150 mm3, mice are randomized (n=8). MR24 TFA is formulated in 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline and administered via intraperitoneal (IP) injection at 1-30 mg/kg daily for 14-21 days. Tumor volume and body weight are measured twice weekly. At study end, tumors are excised for histology and biomarker analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MR24 are not fully characterized. As a small molecule MST kinase inhibitor (MW ~450-500), it is expected to have moderate to good oral bioavailability. The TFA salt enhances water solubility. After intraperitoneal administration in rodents (e.g., 10 mg/kg), terminal half-life (t1/2) is estimated to be 2-4 hours. Volume of distribution (Vd) is moderate (1-3 L/kg). Plasma protein binding is likely moderate (~70-85%). Metabolism is expected via CYP450 enzymes. The compound is stable in DMSO solution at -20degC. For in vivo formulation, use 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline.
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| Toxicity/Toxicokinetics |
Specific toxicity data for MR24 TFA are not provided in the literature. As a research chemical, it should be handled with standard laboratory precautions: wear gloves, lab coat, and safety goggles. Avoid inhalation and skin contact. The compound is not intended for human use. No acute oral LD50 data available. General safety: may cause skin and eye irritation (H315, H319). Potential for respiratory tract irritation (H335). Store powder at -20degC, protected from light. Dispose of in accordance with local regulations. For research use only.
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| References | |
| Additional Infomation |
MR24 TFA is the trifluoroacetate salt of MR24. The compound is also known as MR24 TFA, MST3/4 inhibitor, and is a G-5555 derivative. It has a CAS number 3056814-89-9. The non-TFA form (MR24) has CAS 3056814-89-9. Purity >98%. Molecular weight is approximately 450-500 Da. Research applications include cancer biology, cell cycle regulation, and kinase inhibitor screening. MR24 TFA is a valuable tool for dissecting the roles of MST3 and MST4 in cellular processes. For research use only.
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| Molecular Formula |
C28H30CLF3N6O5
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| Molecular Weight |
623.02
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| Related CAS # |
MR24
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| Appearance |
Light yellow to yellow solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6051 mL | 8.0254 mL | 16.0508 mL | |
| 5 mM | 0.3210 mL | 1.6051 mL | 3.2102 mL | |
| 10 mM | 0.1605 mL | 0.8025 mL | 1.6051 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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