2506273-81-8
Chemical Structure
VT3989
- CAS No.: 2506273-81-8
- Formula:C21H18F3NO3
- Molecular Weight:389.37
InChIKey: FJIVCOAHSKDOAC-CYBMUJFWSA-N
SMILES: OC[C@@H](C)NC(C(C=C1)=CC2=C1C(OC3=CC=C(C=C3)C(F)(F)F)=CC=C2)=O
Biological Activity:
VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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VT3989 | 99.61% | VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors. |
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- [1]. Haddox C L, et al. SAFETY AND EARLY EFFICACY OF VT3989, A TEAD INHIBITOR, IN PATIENTS WITH ADVANCED EPITHELIOID HEMANGIOENDOTHELIOMA (EHE): A PHASE I/II STUDY[J]. ESMO Rare Cancers, 2025, 4.
- [2]. Laws M T, et al. Variable Schwann cell merlin inactivation is targetable with TEAD1 inhibition in schwannomas[J]. bioRxiv, 2025: 2025.11. 15.688608.
- [3]. Tang T T, et al. The TEAD autopalmitoylation inhibitor VT3989 improves efficacy and increases durability of efficacy of osimertinib in preclinical EGFR mutant tumor models[J]. Cancer Research, 2022, 82(12_Supplement): 5364-5364.
- [4]. Koroleva OA, et al. The Hippo pathway as an antitumor target: time to focus on. Expert Opin Investig Drugs. 2024;33(12):1177-1185. [Content Brief]
Keywords
