Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]-
- CAS No.
- 2290608-13-6
- Chemical Name:
- Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]-
- Synonyms
- VT103;VT103, 10 mM in DMSO;N-Methyl-3-(1-methyl-1H-imidazol-4-yl)-4-((4-(trifluoromethyl)phenyl)amino)benzenesulfonamide;Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]-
- CBNumber:
- CB69021479
- Molecular Formula:
- C18H17F3N4O2S
- Molecular Weight:
- 410.41
- MDL Number:
- MFCD34567638
- MOL File:
- 2290608-13-6.mol
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- Properties
Boiling point | 583.6±60.0 °C(Predicted) |
---|---|
Density | 1.39±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | DMSO : 50 mg/mL (121.83 mM; Need ultrasonic) |
pka | 11.55±0.50(Predicted) |
form | Solid |
color | Off-white to gray |
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- Chemical Properties,Uses,Production
Uses
VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer[1].
Biological Activity
VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer[1]. VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP-TEAD1 interaction[1].VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1]. VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1].
in vivo
VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1].
Pharmacokinetics of VT103 in mice[1]
Dose | IV | PO | ||||||
7 mg/kg | T1/2 (hours) | Vdss (L/kg) | CI(mL/min/kg) | AUC 0-24 hours (μg*h/mL) | AUC 0-24 hours (μg*h/mL) | Oral availability (%) | Cmax (ng/mL) | C24 hours (ng/mL) |
13.2 | 4.5 | 4.7 | 20.0 | 14.9 | 75 | 896 (1 hour) | 340 |
Animal Model: | NCI-H226-tumor bearing mice[1] |
Dosage: | 0.3~10 mg/kg |
Administration: | P.o. once per day |
Result: | Blocked tumor growth even at 0.3 mg/kg. |
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;20(6):986-998.
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
Blocksynth Pharmaceutical Technology Co.,Ltd | 0086-19817745290; +8619817745290 | bd@blocksynth.com | China | 5661 | 58 |
Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd. | 21-57721279 | sales@shydchem.com.cn | China | 990 | 56 |
Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71829 | 60 |
Shanghai Chaolan Chemical Technology Center | 021-QQ:65489617 15618227136 | Sales@ATKchemical.com | China | 9330 | 58 |
Heze Development Zone chuangli Chemical Co., Ltd. | 0530-+86-530-529 6766,+86-15666160102 15666160102 | info@chuangli-chem.com | China | 838 | 55 |
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 998 | 58 |
ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4348 | 58 |
JinOu Biomedical (Nanjing) Co., Ltd. | 13000000000 | jinoupharma@163.com | China | 11721 | 58 |
Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62072 | 58 |