| Identification | Back Directory | [Name]
2-Naphthalenecarboxamide, N-[(1S)-1-(2-pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]- | [CAS]
2417718-25-1 | [Synonyms]
VT-104
2-Naphthalenecarboxamide, N-[(1S)-1-(2-pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]- | [Molecular Formula]
C25H19F3N2O | [MOL File]
2417718-25-1.mol | [Molecular Weight]
420.43 |
| Chemical Properties | Back Directory | [Boiling point ]
583.3±50.0 °C(Predicted) | [density ]
1.259±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
13.30±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
VT-104 is a potent and selective TEAD Auto-palmitoylation inhibitor that Inhibits Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT104 is an analog of VT102, which has improved potency and good oral pharmacokinetics in mice. VT104 prevented palmitoylation of the TEAD1 protein. VT104 showed excellent orally bioavailability and long half-lives, which inhibits tumor growth and also lead to shrinkage of established tumors in preclinical models of human mesothelioma CDX models deficient in functional Merlin. | [Uses]
VT104 is a potent and orally active YAP/TAZ inhibitor. VT104 prevents palmitoylation of endogenous TEAD1 and TEAD3 proteins. VT104 can be used in research of cancer[1][2]. | [in vivo]
VT104 (0.3-3 mg/kg; p.o.; NCI-H226-tumor bearing mice) blocks growth of NF2-deficient mesothelioma xenografts[1]. | Animal Model: | NCI-H226-tumor bearing mice[1] | | Dosage: | 0.3, 1, and 3 mg/kg | | Administration: | Oral administration | | Result: | Blocked NCI-H226 tumor growth in mice in dose-dependent manner. |
| [References]
[1] Tang TT, et, al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021 Jun;20(6):986-998. DOI:10.1158/1535-7163.MCT-20-0717
[2] Barry ER, et, al. Recent Therapeutic Approaches to Modulate the Hippo Pathway in Oncology and Regenerative Medicine. Cells. 2021 Oct 11;10(10):2715. DOI:10.3390/cells10102715 |
|
|