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SM16

Cat. No. M9683
SM16 Structure
Synonym:

SM-16

Size Price Availability
10mg USD 211  USD211 4-7 Days
25mg USD 442  USD442 4-7 Days
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Quality Control & Documentation
Biological Activity

SM16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively. SM16 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 i.p. bolus of 20 mg/kg SM16.

Chemical Information
Molecular Weight 430.5
Formula C25H26N4O3
CAS Number 614749-78-9
Solubility (25°C) DMSO ≥ 55 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kristin V T Engebretsen, et al. J Mol Cell Cardiol. Attenuated development of cardiac fibrosis in left ventricular pressure overload by SM16, an orally active inhibitor of ALK5

[2] Kai Fu, et al. Arterioscler Thromb Vasc Biol. SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model

[3] Eiji Suzuki, et al. Cancer Res. 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

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Keywords: SM16, SM-16 supplier, TGF-β Receptor, inhibitors, activators


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