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VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $126 | In Stock | |
5 mg | $313 | In Stock | |
10 mg | $496 | In Stock | |
25 mg | $892 | In Stock | |
50 mg | $1,450 | In Stock | |
100 mg | $1,970 | In Stock | |
1 mL x 10 mM (in DMSO) | $345 | In Stock |
Description | VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer. |
In vitro | VT103 (3 mmol/L; 4 or 24 h; NF2-deficient NCI-H226 cells) selectively disrupts YAP–TEAD1 interaction.[1] VT103 (3 μM; HEK293T cells) appeared to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4.[1] VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT103 shows an IC50 of 1.02 nM in the YAP reporter assay.[1] |
In vivo | VT103 (0.3~10 mg/kg; p.o.; once daily; NCI-H226-tumor-bearing mice) inhibits tumor growth, with efficacy observed at 0.3 mg/kg[1]. Pharmacokinetics of VT103 in mice.[1] |
Alias | VT-103, VT 103 |
Molecular Weight | 410.41 |
Formula | C18H17F3N4O2S |
Cas No. | 2290608-13-6 |
Smiles | CNS(=O)(=O)c1ccc(Nc2ccc(cc2)C(F)(F)F)c(c1)-c1cn(C)cn1 |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (121.83 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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