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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 | Availability | 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 | TNF-α secretion (Raw cells):40 nM, ADAM12:1.8 nM(ki), MMP14:26 nM, ADAM17/TACE:8.4 nM (IC50), ADAMTS-4:100 nM, ADAM10:16 nM(ki), MMP13:3 nM, MMP9:12 nM, TNF-α secretion (THP-1 cells):200 nM, ADAM17/TACE:0.079 nM(ki), MMP1:6.6 nM, MMP2:4.7 nM, ADAM8:21 nM(ki), MMP7:26 nM |
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] |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 35.9 mg/mL (410.4 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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