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MedKoo Cat#: 408142 | Name: VT-104
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

VT-104
VT-104
CAS#2417718-25-1 (S-isomer)

Theoretical Analysis

MedKoo Cat#: 408142

Name: VT-104

CAS#: 2417718-25-1 (S-isomer)

Chemical Formula: C25H19F3N2O

Exact Mass: 420.1449

Molecular Weight: 420.44

Elemental Analysis: C, 71.42; H, 4.56; F, 13.56; N, 6.66; O, 3.81

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
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Related CAS #
2417718-25-1 (S-isomer) 2417718-26-2 (R-isomer) 2417720-80-8 (racemate)
Synonym
VT-104; VT 104; VT104
IUPAC/Chemical Name
(S)-N-(1-(pyridin-2-yl)ethyl)-5-(4-(trifluoromethyl)phenyl)-2-naphthamide
InChi Key
AAZUPSFRSHFTGV-INIZCTEOSA-N
InChi Code
InChI=1S/C25H19F3N2O/c1-16(23-7-2-3-14-29-23)30-24(31)19-10-13-22-18(15-19)5-4-6-21(22)17-8-11-20(12-9-17)25(26,27)28/h2-16H,1H3,(H,30,31)/t16-/m0/s1
SMILES Code
FC(F)(F)C(C=C1)=CC=C1C2=CC=CC3=CC(C(N[C@@H](C)C4=NC=CC=C4)=O)=CC=C23
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
VT104 inhibits TEAD-mediated gene transcription (IC50 = 10.4 nM), and is an NF2 inhibitor (NCI-H2051 IC50 = 31.6 nM)
In vitro activity:
Combination therapy with VT104 and EGFR-TKIs showed better tumor-suppressive effects than EGFR-TKIs alone, in vitro and in vivo. Moreover, the combined effect of VT104 and EGFR-TKIs was observed regardless of the localization status of YAP1 before EGFR-TKI exposure. Reference: Ogimoto T, Ozasa H, Tsuji T, Funazo T, Yamazoe M, Hashimoto K, Yoshida H, Hosoya K, Ajimizu H, Nomizo T, Yoshida H, Hamaji M, Menju T, Yoshizawa A, Date H, Hirai T. Combination Therapy with EGFR Tyrosine Kinase Inhibitors and TEAD Inhibitor Increases Tumor Suppression Effects in EGFR Mutation-positive Lung Cancer. Mol Cancer Ther. 2024 Apr 2;23(4):564-576. doi: 10.1158/1535-7163.MCT-23-0371. PMID: 38052760.
In vivo activity:
Combination therapy with VT104 and EGFR-TKIs showed better tumor-suppressive effects than EGFR-TKIs alone, in vitro and in vivo. Moreover, the combined effect of VT104 and EGFR-TKIs was observed regardless of the localization status of YAP1 before EGFR-TKI exposure. Reference: Ogimoto T, Ozasa H, Tsuji T, Funazo T, Yamazoe M, Hashimoto K, Yoshida H, Hosoya K, Ajimizu H, Nomizo T, Yoshida H, Hamaji M, Menju T, Yoshizawa A, Date H, Hirai T. Combination Therapy with EGFR Tyrosine Kinase Inhibitors and TEAD Inhibitor Increases Tumor Suppression Effects in EGFR Mutation-positive Lung Cancer. Mol Cancer Ther. 2024 Apr 2;23(4):564-576. doi: 10.1158/1535-7163.MCT-23-0371. PMID: 38052760.
Solvent mg/mL mM
Solubility
DMSO 100.0 237.85
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 420.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1: Ogimoto T, Ozasa H, Tsuji T, Funazo T, Yamazoe M, Hashimoto K, Yoshida H, Hosoya K, Ajimizu H, Nomizo T, Yoshida H, Hamaji M, Menju T, Yoshizawa A, Date H, Hirai T. Combination Therapy with EGFR Tyrosine Kinase Inhibitors and TEAD Inhibitor Increases Tumor Suppression Effects in EGFR Mutation-positive Lung Cancer. Mol Cancer Ther. 2024 Apr 2;23(4):564-576. doi: 10.1158/1535-7163.MCT-23-0371. PMID: 38052760.
In vivo protocol:
1: Ogimoto T, Ozasa H, Tsuji T, Funazo T, Yamazoe M, Hashimoto K, Yoshida H, Hosoya K, Ajimizu H, Nomizo T, Yoshida H, Hamaji M, Menju T, Yoshizawa A, Date H, Hirai T. Combination Therapy with EGFR Tyrosine Kinase Inhibitors and TEAD Inhibitor Increases Tumor Suppression Effects in EGFR Mutation-positive Lung Cancer. Mol Cancer Ther. 2024 Apr 2;23(4):564-576. doi: 10.1158/1535-7163.MCT-23-0371. PMID: 38052760. 2: Uccioli L, Magnani P, Tilli P, Cotroneo P, Manto A, Greco AV, Sima AA, Greene DA, Menzinger G, Ghirlanda G. Abnormal agonist-stimulated cardiac parasympathetic acetylcholine release in streptozocin-induced diabetes. Diabetes. 1993 Jan;42(1):141-7. doi: 10.2337/diab.42.1.141. PMID: 8093604.
Lopez K, Deng JJ, Xu Y, Sharkey FE, Wang P, Liu J. Exploring the Role of YAP1 and TAZ in Pancreatic Acinar Cells and the Therapeutic Potential of VT-104 in Pancreatic Inflammation. bioRxiv [Preprint]. 2023 Sep 18:2023.09.18.558321. doi: 10.1101/2023.09.18.558321. PMID: 37781601; PMCID: PMC10541090.