WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408141
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.
MedKoo Cat#: 408141
Chemical Formula: C18H17F3N4O2S
Exact Mass: 410.1024
Molecular Weight: 410.42
Elemental Analysis: C, 52.68; H, 4.18; F, 13.89; N, 13.65; O, 7.80; S, 7.81
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.
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
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.
|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|
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.