| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Endogenous TEAD1 and TEAD3 phospholipids are inhibited by VT107 (3 μmol/L; 20 hours; HEK293T cells) and endogenous TEAD4 phospholipids are efficiently inhibited as well [1]. On TEAD2 and TEAD4, VT107 is somewhat more potent than VT104. The removal of thermoplastic TEAD1 was produced by VT107, but it did not increase thermoplastic TEAD1. The thermoplastics TEAD3 and TEAD4 are decreased in VT107 without being increased in VT107. Additionally, VT107 prevents YAP and TAZ from reacting with TEAD1 and TEAD4. VT107 efficiently prevents NF2 mutant or defective cell lines from proliferating [1].
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|---|---|
| ln Vivo |
VT107 (10 mg/kg; po) is an enantiomeric analog of VT104 [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T Cell Tested Concentrations: 3 μmol/L Incubation Duration: 20 hrs (hours) Experimental Results: Inhibited palmitoylation of endogenous TEAD1 and TEAD3 proteins, and most effectively blocked palmitoylation of endogenous TEAD4 protein . |
| Animal Protocol |
Animal/Disease Models: Mouse[1]
Doses: 10 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Po Experimental Results: Similar enantiomer to VT104. |
| References |
| Molecular Formula |
C25H20F3N3O
|
|---|---|
| Molecular Weight |
435.44
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| Exact Mass |
435.155
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| CAS # |
2417718-63-7
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| Related CAS # |
2417718-63-7 (S-isomer);2417718-64-8 (R-isomer);2417720-81-9 (Racemate);
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| PubChem CID |
153583246
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
634
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(C(=O)N[C@@H](C)C2N=C(C=CC=2)N)=CC=C2C(C3C=CC(C(F)(F)F)=CC=3)=CC=CC2=C1
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| InChi Key |
OBEXKSHQMHIUFP-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C25H20F3N3O/c1-15(22-6-3-7-23(29)31-22)30-24(32)18-10-13-21-17(14-18)4-2-5-20(21)16-8-11-19(12-9-16)25(26,27)28/h2-15H,1H3,(H2,29,31)(H,30,32)/t15-/m0/s1
|
| Chemical Name |
N-[(1S)-1-(6-aminopyridin-2-yl)ethyl]-5-[4-(trifluoromethyl)phenyl]naphthalene-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~229.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2965 mL | 11.4826 mL | 22.9653 mL | |
| 5 mM | 0.4593 mL | 2.2965 mL | 4.5931 mL | |
| 10 mM | 0.2297 mL | 1.1483 mL | 2.2965 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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