MYF-03-176
Based on 1 publication(s) in Google Scholar
MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model.
For research use only. We do not sell to patients.
- Purity : 99.72%
- CAS No.: 2857937-59-6
- Formula: C19H18F4N4O2
- Molecular Weight:410.37
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MYF-03-176
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Biological Activity
Description
IC50 & Target
IC50: TEAD1 (47 nM), TEAD2 (275 nM), TEAD3 (32 nM), TEAD4 (71 nM)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NCI-H226 | IC50 |
24 nM
Compound: 22
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Antiproliferative activity against human NCI-H226 cells assessed as reduction in cell viability measured for 5 days by celliter-glo assay
Antiproliferative activity against human NCI-H226 cells assessed as reduction in cell viability measured for 5 days by celliter-glo assay
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[PMID: 36946421] |
In Vitro
MYF-03-176 (10-4-100 μM, 72 h) inhibits TEAD transcriptional activity with an IC50 of 11 nM in NCI-H226 cells[1].
MYF-03-176 (20-500 nM, 24 h) leads to a significant down-regulation of YAP target genes CTGF, CYR61, ANKRD1 and an up-regulation of BMF, indicating it inhibits Hippo signaling defective MPM cells[1].
MYF-03-176 (0-104 nM, 5 days) inhibits the growth of NCI-H226 cells with an IC50 of 9 nM[1].
MYF-03-176 (0-5 μM, 10-14 d) exhibits extraordinarily synergistic effects with KRAS G12C and KRAS G12D inhibitors in multiple cell lines[3].
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:H358, H358R N20, H358R, KYSE410, SW1573, H2030, H1373 YAP S127A, HPAFII, HPAFIIR, PANC1, and SW1990 cells
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Concentration:0.5, 1, 5 μM (H358, H358R N20, H358R, SW1573, HPAFII, HPAFIIR, PANC1, SW1990); 50, 100, 500 nM (KYSE410, H2030 cells); 5, 10, 15 μM (SW1573, H2030, H1373 YAP S127A)
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Incubation Time:10-14 d
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Result:Exhibited extraordinarily synergistic effects with KRAS G12C and KRAS G12D inhibitors.
In Vivo
MYF-03-176 (100 mg/kg; p.o.; twice daily for 21 days) reduces the tumor volumes when in combination with AMG510 (KRAS G12C inhibitor) (HY-114277), without affecting body weight in SW1753 xenograft BALB/c nude mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (6-8 weeks) (inoculated with SW1573 (1 x 107) cells in the right flank)[3]
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Dosage:100 mg/kg
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Administration:Oral gavage (p.o.); twice daily for 21 days
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Result:Reduced the tumor volumes when in combination with AMG510 (KRAS G12C inhibitor), without affecting body weight.
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Animal Model:Female 7-week-old NSG mice (5×106 cells were implanted subcutaneously in the right flan)[1]
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Dosage:30, 75 mg/kg
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Administration:Oral gavage (p.o.); twice daily for 28 days
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Result:Significant antitumor activity with tumor regressions was observed at both 30 mg/kg (average tumor regression of 54%) and 75 mg/kg (average tumor regression of 68%).
At 75 mg/kg dose, three of eight animals demonstrated 12-14% body weight loss. The weight loss recovered once drug administration was stopped.
Chemical Information
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CAS No. 2857937-59-6
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Appearance Solid
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Molecular Weight 410.37
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Formula C19H18F4N4O2
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Color White to off-white
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SMILES
FC(F)(F)C1=CC=C(CO[C@@H]2CN(C(C(F)=C)=O)C[C@H]2NC3=NC=CC=N3)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Cell
2025 Sep 18;85(18):3425-3442.e10. PMID: 40914169
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (243.68 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Protocols
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[2]. Lu W, et al. Structure-Based Design of Y-Shaped Covalent TEAD Inhibitors. J Med Chem. 2023 Apr 13;66(7):4617-4632. [Content Brief]
[3]. Yang W, et al. YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. JCI Insight. 2024 Dec 20;9(24):e178535. [Content Brief]
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 (sealed storage, away from moisture and light). 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 | 2.4368 mL | 12.1841 mL | 24.3683 mL | 60.9206 mL |
| 5 mM | 0.4874 mL | 2.4368 mL | 4.8737 mL | 12.1841 mL | |
| 10 mM | 0.2437 mL | 1.2184 mL | 2.4368 mL | 6.0921 mL | |
| 15 mM | 0.1625 mL | 0.8123 mL | 1.6246 mL | 4.0614 mL | |
| 20 mM | 0.1218 mL | 0.6092 mL | 1.2184 mL | 3.0460 mL | |
| 25 mM | 0.0975 mL | 0.4874 mL | 0.9747 mL | 2.4368 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8123 mL | 2.0307 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5230 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4874 mL | 1.2184 mL | |
| 60 mM | 0.0406 mL | 0.2031 mL | 0.4061 mL | 1.0153 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6092 mL |
MYF-03-176 Related Classifications
HY-147136 Related Classifications
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