| Identification | Back Directory | [Name]
SM16 | [CAS]
614749-78-9 | [Synonyms]
SM16
CS-2835
4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide
Bicyclo[2.2.2]octane-1-carboxamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]- | [Molecular Formula]
C25H26N4O3 | [MOL File]
614749-78-9.mol | [Molecular Weight]
430.5 |
| Chemical Properties | Back Directory | [Boiling point ]
691.3±55.0 °C(Predicted) | [density ]
1.354±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:65.0(Max Conc. mg/mL);150.99(Max Conc. mM) | [form ]
A solid | [pka]
11.23±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively. | [Biological Activity]
SM 16 is an ALK5/ALK4 kinase inhibitor with Ki values of 10 and 1.5 nM, respectively. | [in vivo]
SM 16 penetrates tumor cells in vivo , suppressing tumor phosphorylated Smad2/3 levels for at least 3 h following treatment of tumor-bearing mice with a single ip bolus of 20 mg/kg SM 16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P<0.001) delivered via sc miniosmotic pumps over 28 days. < /p> | [target]
Ki: ALK5 (10 nM), ALK4 (1.5 nM) | [storage]
Store at -20°C | [References]
[1] Suzuki E, et al. A novel small-molecule inhibitor of transforming growth factor beta type I receptor kinase (SM16) inhibits murine mesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection. Cancer Res. 2007 Mar 1;67(5):2351-9. DOI:10.1158/0008-5472.CAN-06-2389
[2] Fu K, et al. SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model. Arterioscler Thromb Vasc Biol. 2008 Apr;28(4):665-71. DOI:10.1161/ATVBAHA.107.158030
[3] Engebretsen KV, et al. Attenuated development of cardiac fibrosis in left ventricular pressure overload by SM16, an orally active inhibitor of ALK5. J Mol Cell Cardiol. 2014 Nov;76:148-57. DOI:10.1016/j.yjmcc.2014.08.008 |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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