VT103, a VT101 analog, is a selective and orally active TEAD1 protein palmitoylation inhibitor that can be used in cancer research. VT103 inhibits the transcription of YAP/TAZ-TEAD promoted gene, blocks the auto-palmitoylation of TEAD, and interferes with the interaction between YAP/TAZ and TEAD.
| Molecular Weight | 410.41 |
| Formula | C18H17F3N4O2S |
| CAS Number | 2290608-13-6 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related YAP Products |
|---|
| VT3989
VT3989 is a first-in-class, orally active, potent and selective YAP/TEAD auto-palmitoylation inhibitor. VT3989 works by inhibiting TEAD palmitoylation, which in turn blocks YAP function. |
| YAP-TEAD-IN-1
YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). |
| YAP-TEAD-IN-3
YAP-TEAD-IN-3 is a YAP/TAZ-TEAD inhibitor. |
| Lappaol F
Lappaol F, a lignin, is an anticancer agent. |
| IK-930
IK-930 is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM. |
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