2. Stem Cell/Wnt
  3. YAP
  4. VT103

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.

For research use only. We do not sell to patients.

VT103 Chemical Structure

VT103 Chemical Structure

CAS No. : 2290608-13-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 418 In-stock
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 600 In-stock
25 mg USD 1100 In-stock
50 mg USD 1760 In-stock
100 mg USD 2800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

VT103 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer[1].

IC50 & Target

TEAD1 Palmitoylation[1]
Cellular Effect
Cell Line Type Value Description References
NCI-H226 IC50
0.003 μM
Compound: VT-103
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

VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction[1].
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1].
VT103 shows an IC50 of 1.02 nM in YAP reporter assay[1].

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

VT103 Related Antibodies
In Vivo

VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1].
Pharmacokinetics of VT103 in mice[1]

Dose IV PO
7 mg/kg T1/2 (hours) Vdss (L/kg) CI(mL/min/kg) AUC 0-24 hours (μg*h/mL) AUC 0-24 hours (μg*h/mL) Oral availability (%) Cmax (ng/mL) C24 hours (ng/mL)
13.2 4.5 4.7 20.0 14.9 75 896 (1 hour) 340

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

Animal Model: NCI-H226-tumor bearing mice[1]
Dosage: 0.3~10 mg/kg
Administration: P.o. once per day
Result: Blocked tumor growth even at 0.3 mg/kg.
Molecular Weight

410.41

Formula

C18H17F3N4O2S
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=S(C1=CC=C(NC2=CC=C(C(F)(F)F)C=C2)C(C3=CN(C)C=N3)=C1)(NC)=O
Shipping

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

DMSO : 50 mg/mL (121.83 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 2.4366 mL 12.1829 mL 24.3659 mL
5 mM 0.4873 mL 2.4366 mL 4.8732 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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

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Volume (start)

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C2

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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    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:
%
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: 99.26%

SDS (252 KB)

COA (253 KB) HNMR (113 KB) RP-HPLC (330 KB) MS (104 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4366 mL 12.1829 mL 24.3659 mL 60.9147 mL
5 mM 0.4873 mL 2.4366 mL 4.8732 mL 12.1829 mL
10 mM 0.2437 mL 1.2183 mL 2.4366 mL 6.0915 mL
15 mM 0.1624 mL 0.8122 mL 1.6244 mL 4.0610 mL
20 mM 0.1218 mL 0.6091 mL 1.2183 mL 3.0457 mL
25 mM 0.0975 mL 0.4873 mL 0.9746 mL 2.4366 mL
30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0305 mL
40 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5229 mL
50 mM 0.0487 mL 0.2437 mL 0.4873 mL 1.2183 mL
60 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
100 mM 0.0244 mL 0.1218 mL 0.2437 mL 0.6091 mL
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VT103 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:

VT1032290608-13-6VT 103VT-103YAPYes-associated proteinVT101palmitoylationcancerHEK293TNCI-H226NF2unpalmitoylatedTAPTAZInhibitorinhibitorinhibit

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