2. Stem Cell/Wnt
  3. YAP
  4. GNE-7883

GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation.

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GNE-7883 Chemical Structure

GNE-7883 Chemical Structure

CAS No. : 2648450-42-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 396 In-stock
Solution
10 mM * 1 mL in DMSO USD 396 In-stock
Solid
1 mg USD 144 In-stock
5 mg USD 360 In-stock
10 mg USD 580 In-stock
50 mg USD 1560 In-stock
100 mg USD 2500 In-stock
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Based on 1 publication(s) in Google Scholar

GNE-7883 Related Antibodies

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  • Purity & Documentation

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Description

GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation[1][2][3].

IC50 & Target

TEAD[1].
Cellular Effect
Cell Line Type Value Description References
NCI-H226 IC50
0.082 μM
Compound: GNE-7883
Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
[PMID: 35763499]
In Vitro

GNE-7883 exhibits strong dose-dependent antiproliferative effects in both OVCAR-8 and NCI-H226 cells, with EC50 values ​​of 115 nM and 333 nM, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GNE-7883 Related Antibodies
In Vivo

GNE-7883 (100 and 250 mg/kg; s.c.; once daily for 4 days) induces tumor growth arrest in NCI-H226 xenograft mice and tumor regression in MSTO-211H xenograft mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mesothelioma NCIH226 xenograft mouse model[3]
Dosage: 250 mg/kg
Administration: Subcutaneous injection (s.c.); Once a day for 4 days
Result: Had a strong inhibitory effect on tumor growth in vivo, with an inhibition rate of 102%.
Molecular Weight

500.57

Formula

C28H29FN6O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C=C(C1=CC=C(C2CCCCC2)C=C1)N3)N4C3=C(C(N5CC(CF)C5)=O)C(C6=NC=CN=C6C)=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (99.89 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 1.9977 mL 9.9886 mL 19.9772 mL
5 mM 0.3995 mL 1.9977 mL 3.9954 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.99 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.99 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:
%
DMSO +
% 
+
%
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).
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

Purity: 98.49%

SDS (251 KB)

COA (250 KB) HNMR (265 KB) LCMS (93 KB)

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 1.9977 mL 9.9886 mL 19.9772 mL 49.9431 mL
5 mM 0.3995 mL 1.9977 mL 3.9954 mL 9.9886 mL
10 mM 0.1998 mL 0.9989 mL 1.9977 mL 4.9943 mL
15 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3295 mL
20 mM 0.0999 mL 0.4994 mL 0.9989 mL 2.4972 mL
25 mM 0.0799 mL 0.3995 mL 0.7991 mL 1.9977 mL
30 mM 0.0666 mL 0.3330 mL 0.6659 mL 1.6648 mL
40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2486 mL
50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9989 mL
60 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8324 mL
80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
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GNE-7883 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:

GNE-78832648450-42-2GNE7883GNE 7883YAPYes-associated proteincell proliferationcancerYAP/TAZInhibitorinhibitorinhibit

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