2. Stem Cell/Wnt
  3. YAP
  4. MYF-03-176

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.

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MYF-03-176 Chemical Structure

MYF-03-176 Chemical Structure

CAS No. : 2857937-59-6

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Based on 1 publication(s) in Google Scholar

MYF-03-176 Related Antibodies

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Description

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[1][2][3].

IC50 & Target

IC50: TEAD1 (47 nM), TEAD2 (275 nM), TEAD3 IC50 (32 nM), TEAD4 IC50 (71 nM)
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.

MYF-03-176 Related Antibodies

Cell Proliferation Assay[3]

Cell Line: H358, H358R N20, H358R, KYSE410, SW1573, H2030, H1373 YAP S127A, HPAFII, HPAFIIR, PANC1, and SW1990 cells
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)
Incubation Time: 10-14 d
Result: Exhibited extraordinarily synergistic effects with KRAS G12C and KRAS G12D inhibitors.
In Vivo

MYF-03-176 (30-75 mg/kg; p.o.; twice daily for 28 days) exhibits strong antitumor effect in the human mesothelioma NCI-H226 CDX model in vivo[1].
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.

Animal Model: Female BALB/c nude mice (6-8 weeks) (inoculated with SW1573 (1 x 107) cells in the right flank)[3]
Dosage: 100 mg/kg
Administration: Oral gavage (p.o.); twice daily for 21 days
Result: Reduced the tumor volumes when in combination with AMG510 (KRAS G12C inhibitor), without affecting body weight.
Animal Model: Female 7-week-old NSG mice (5×106 cells were implanted subcutaneously in the right flan)[1]
Dosage: 30, 75 mg/kg
Administration: Oral gavage (p.o.); twice daily for 28 days
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.
Molecular Weight

410.37

Formula

C19H18F4N4O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4368 mL 12.1841 mL 24.3683 mL
5 mM 0.4874 mL 2.4368 mL 4.8737 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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 (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
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MYF-03-176 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MYF-03-1762857937-59-6YAPYes-associated proteinorally activeanticancerInhibitorinhibitorinhibit

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