VT-103
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MedKoo CAT#: 408141

CAS#: 2290608-13-6

Description: VT-103 is a potent and selective TEAD Auto-palmitoylation inhibitor that Inhibits Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT103 is a TEAD1-selective inhibitor. VT103 is an analog of VT101, which has 238 improved potency and good oral pharmacokinetics in mice. VT103 selectively inhibited endogenous TEAD1 palmitoylation in cells. VT103 significantly downregulated the expression of the Hippo pathway target genes, CTGF and CYR61, in the NF2-deficient NCI-H226 tumors in mice in a dose-dependent manner. VT103 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

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VT-103
CAS# 2290608-13-6
Instruction

Theoretical Analysis

MedKoo Cat#: 408141
Name: VT-103
CAS#: 2290608-13-6
Chemical Formula: C18H17F3N4O2S
Exact Mass: 410.10
Molecular Weight: 410.420
Elemental Analysis: C, 52.68; H, 4.18; F, 13.89; N, 13.65; O, 7.80; S, 7.81

Price and Availability

Size Price Availability Quantity
5mg USD 750 2 Weeks
25mg USD 1650 2 Weeks
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Synonym: VT-103; VT 103; VT103

IUPAC/Chemical Name: N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-((4-(trifluoromethyl)phenyl)amino)benzenesulfonamide

InChi Key: LLCVDQHLYHBAHR-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H17F3N4O2S/c1-22-28(26,27)14-7-8-16(15(9-14)17-10-25(2)11-23-17)24-13-5-3-12(4-6-13)18(19,20)21/h3-11,22,24H,1-2H3

SMILES Code: CN1C=NC(C2=C(NC3=CC=C(C(F)(F)F)C=C3)C=CC(S(=O)(NC)=O)=C2)=C1

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:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 410.42 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:
In vivo protocol:

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Tang TT, Konradi AW, Feng Y, Peng X, Ma M, Li J, Yu FX, Guan KL, Post L. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021 Apr 13:molcanther.0717.2020. doi: 10.1158/1535-7163.MCT-20-0717. Epub ahead of print. PMID: 33850002.