1. Stem Cell/Wnt
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  3. VT103

VT103 

Cat. No.: HY-134955 Purity: 98.63%
Handling Instructions

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
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 Get quote
100 mg USD 3400 Get quote
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Based on 1 publication(s) in Google Scholar

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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]

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].

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

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

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.
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 (121.83 mM; Need ultrasonic)

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
10 mM 0.2437 mL 1.2183 mL 2.4366 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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