2290608-13-6
2290608-13-6 structure
- Name: VT103
- Chemical Name: VT103
- CAS Number: 2290608-13-6
- Molecular Formula: C18H17F3N4O2S
- Molecular Weight: 410.41
- Catalog: Signaling Pathways Stem Cell/Wnt YAP
- Create Date: 2022-01-11 12:24:24
- Modify Date: 2024-01-09 11:59:55
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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].
| Name | VT103 |
|---|
| 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]. |
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| Related Catalog | |
| 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]. |
| 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 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. |
| References |
| Molecular Formula | C18H17F3N4O2S |
|---|---|
| Molecular Weight | 410.41 |