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Purity: ≥98%
SD-208 (SD208; SD 208; TGF-β RI Kinase Inhibitor V) is an orally bioavailable and selective TGF-βRI (ALK5) inhibitor with potential antitumor activity. It inhibits ALK5 with an IC50 of 48 nM, and displayed >100-fold selectivity for TGF-βRI over TGF-βRII. It shows potent anti-proliferative activity in vitro against various cancer cell lines such as murine and human glioma cells.
| ln Vitro |
In both human LN-308 and murine SMA-560 glioma cells, SD-208 increases immunogenicity while blocking constitutive, TGF-beta-evoked, and cell growth[1]. In vitro, SD-208 promotes migration, invasiveness, and epithelial-to-mesenchymal transdifferentiation through blocking TGF-beta-induced phosphorylation of Smad2 and Smad3[2]. Additionally, TGF-β's stimulating influence on the migration and proliferation of neointimal smooth muscle-like cells (SMLCs) in vitro is eliminated by SD-208[3].
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| ln Vivo |
Mice bearing SMA-560 gliomas have a considerably longer median survival when treated with SD-208 (1 mg/mL, po)[1]. SD-208 (60 mg/kg/d, po) prevents the formation of primary R3T tumors in syngeneic 129S1 mice and decreases the quantity and size of lung metastases[2]. SD-208 successfully inhibits the development of intimal hyperplasia of transplant arteriosclerosis (TA) in the mouse aortic allograft model[3].
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| References |
[1]. Uhl M, et al. SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 2004 Nov 1;64(21):7954-61.
[2]. Ge R, et al. Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30. [3]. Sun Y, et al. Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208. J Heart Lung Transplant. 2014 Jun;33(6):654-61 |
| Molecular Formula |
C17H10CLFN6
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| Molecular Weight |
352.75
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| CAS # |
627536-09-8
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| SMILES |
FC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2
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| Chemical Name |
2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine
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| Synonyms |
SD-208; SD 208; TGF-β RI Kinase Inhibitor V; SD208;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.91 mg/mL (2.58 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 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: 0.91 mg/mL (2.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 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: ≥ 0.91 mg/mL (2.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% methylcellulose:8 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8349 mL | 14.1743 mL | 28.3487 mL | |
| 5 mM | 0.5670 mL | 2.8349 mL | 5.6697 mL | |
| 10 mM | 0.2835 mL | 1.4174 mL | 2.8349 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.
 A,effects of TβRI kinase inhibitor on anchorage-dependent growth.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. |
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Effects of SD-208 on R3T and 4T1 mammary carcinomasin vivo.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. |
Mechanisms of action of SD-208in vivo.Clin Cancer Res.2006 Jul 15;12(14 Pt 1):4315-30. |
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