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TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $35 | - | In Stock | |
| 5 mg | $81 | - | In Stock | |
| 10 mg | $143 | - | In Stock | |
| 25 mg | $238 | - | In Stock | |
| 50 mg | $357 | - | In Stock | |
| 100 mg | $529 | - | In Stock |
| Description | TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer. |
| Targets&IC50 | ADAM8:21 nM(ki), ADAM12:1.8 nM(ki), MMP14:26 nM, MMP13:3 nM, MMP7:26 nM, ADAM17/TACE:8.4 nM (IC50), TNF-α secretion (Raw cells):40 nM, MMP1:6.6 nM, MMP9:12 nM, ADAM17/TACE:0.079 nM(ki), MMP2:4.7 nM, TNF-α secretion (THP-1 cells):200 nM, ADAMTS-4:100 nM, ADAM10:16 nM(ki) |
| In vitro | TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC50s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC50s = 190 and 300 nM, respectively).[1] It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC50 values of less than 100 nM without inhibiting TNF-α expression in vitro.[3] |
| In vivo | TMI 1 inhibits LPS-induced TNF-α production in mice (ED50 = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED50s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.[3] |
| Synonyms | WAY-171318 |
| Molecular Weight | 398.5 |
| Formula | C17H22N2O5S2 |
| Cas No. | 287403-39-8 |
| Smiles | CC#CCOc1ccc(cc1)S(=O)(=O)N1CCSC(C)(C)[C@@H]1C(=O)NO |
| Relative Density. | 1.325 g/cm3 (Predicted) |
| Storage | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 35.9 mg/mL (90.09 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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