Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
SM16 is a novel and potent Type I TGF-β signaling inhibitor, also a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
ln Vitro |
At doses ranging from 100 to 620 nM, SM 16 suppresses both TGFβ- and activin-induced Smad2 phosphorylation as well as TGFβ-induced plasminogen activator dye luciferase activity (IC50=64 nM). Only SM 16 was tested against p38/SAPKa (IC50=0.8 μM) and Raf (IC50=1 μM) out of over 60 relevant and relevant factors. ALK1 and ALK6, members of the ALK family, are not inhibited by SM 16 [1].
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ln Vivo |
A single intraperitoneal bolus dose of 20 mg/kg SM 16 decreases tumor phosphorylated Smad2/3 levels within tumor cells for a minimum of three hours following treatment of tumor-bearing cells. Subcutaneous microosmotic pump solution 5 mg/kg/d SM 16 (P<0.001) at 28 seconds substantially reduced established AB12 tumors [1].
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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.
[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. [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 |
Molecular Formula |
C25H26N4O3
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Molecular Weight |
430.498945713043
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CAS # |
614749-78-9
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Related CAS # |
614749-78-9
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SMILES |
O=C(C12CCC(C3=NC(C4=CC=C5C(=C4)OCO5)=C(C4C=CC=C(C)N=4)N3)(CC1)CC2)N
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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 : ~65 mg/mL (~150.99 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (5.99 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 25.8 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: ≥ 2.58 mg/mL (5.99 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 25.8 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: ≥ 2.58 mg/mL (5.99 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 | 2.3229 mL | 11.6144 mL | 23.2288 mL | |
5 mM | 0.4646 mL | 2.3229 mL | 4.6458 mL | |
10 mM | 0.2323 mL | 1.1614 mL | 2.3229 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.