| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C17H10ClFN6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SD-208 is a selective inhibitor of TGF-βRI (ALK5), acting with an IC50 of 48 nM and showing more than 100-fold selectivity over TGF-βRII. It is supplied as a light yellow to yellow solid (C17H10ClFN6, MW 352.75) at 99.44% purity.
Physical & Chemical Properties
| CAS Number | 627536-09-8 |
|---|---|
| Molecular Formula | C17H10ClFN6 |
| Molecular Weight | 352.75 g/mol |
| Purity | 99.44% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | FC1=CC=C(Cl)C=C1C2=NC3=NC=CN=C3C(NC4=CC=NC=C4)=N2 |
| Signaling Pathway | TGF-beta/Smad |
| Solubility | In Vitro: DMSO: 9.09 mg/mL (25.77 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 48 nM (TGF-βRI)
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 9.09 mg/mL (25.77 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 0.91 mg/mL (2.58 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 0.91 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (9.1 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 0.91 mg/mL (2.58 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 0.91 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (9.1 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 0.91 mg/mL (2.58 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.91 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (9.1 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | 50% PEG300 + 50% saline |
|---|---|
| Result | 5 mg/mL (14.17 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
In murine SMA-560 and human LN-308 glioma cells, SD-208 inhibits cell growth as well as constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity[1]. SD-208 prevents TGF-beta-induced phosphorylation of Smad2 and Smad3, the receptor-associated Smads, and promotes epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro[2]. SD-208 further abolishes the promoting effect of TGF-β on proliferation and migration of neointimal smooth muscle-like cells (SMLC) in vitro[3].
In Vivo
SD-208 (1 mg/mL, p.o.) significantly extends median survival in SMA-560 glioma-bearing mice[1]. In syngeneic 129S1 mice, SD-208 (60 mg/kg/d, p.o.) suppresses primary R3T tumor growth and decreases both the number and size of lung metastases[2]. SD-208 effectively lowers intimal hyperplasia formation in transplant arteriosclerosis (TA) in the murine aortic allograft model[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Measure kinase activities by the incorporation of radiolabeled ATP into a peptide or protein substrate. Run the reactions in 96-well plates containing the relevant kinase, substrate, ATP, and appropriate cofactors. Incubate the reactions, then stop them by adding phosphoric acid. Capture the substrate on a phosphocellulose filter and wash away unreacted ATP. Determine the incorporated counts with a microplate scintillation counter. Assess the ability of SD-208 to inhibit each kinase by comparing counts incorporated with compound against counts incorporated without compound.
Cell Assay[1]
Culture glioma cells with or without SD-208 (1 μM) for 48 hours. Pulse the cells with [methyl-3H]thymidine (0.5 μCi) for the last 24 hours, harvest them, and determine incorporated radioactivity in a liquid scintillation counter.
Animal Administration[1]
Purchase VM/Dk mice from the TSE Resource Center. Use mice 6 to 12 weeks of age for the survival experiments. Anesthetize groups of eight mice before all intracranial procedures and place them in a stereotaxic fixation device. Drill a burr hole in the skull 2 mm lateral to the bregma. Introduce the needle of a Hamilton syringe to a depth of 3 mm. Inject SMA-560 cells [5×103cells] resuspended in 2 μL of PBS into the right striatum. Three days later, allow the mice to drink SD-208 at 1 mg/mL in deionized water. Observe the mice daily and, in the survival experiments, sacrifice them on development of neurologic symptoms.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Ovarian cancer-derived TGF-β1 induces cancer-associated adipocytes formation by activating SMAD3/TRIB3 pathway to establish pre-metastatic niche. Cell Death Dis 2024 Dec 24;15(12):930. PMID: 39719444
Cell Rep. 2020 Apr.
Upregulation of GLT25D1 in Hepatic Stellate Cells Promotes Liver Fibrosis via the TGF-β1/SMAD3 Pathway In Vivo and In vitro. J Clin Transl Hepatol 2023 Feb 28;11(1):1-14. PMID: 36406310
Nemo-like kinase modulates glucocorticoid-induced erythroid progenitor differentiation by regulating stability of the glucocorticoid receptor. FEBS J 2026 Feb 2. PMID: 41629744
TGF-β1 sustains germ cell cyst reservoir via restraining follicle formation in the chicken. Cell Biol Int 2020 Mar;44(3):861-872.
Astrocyte-Derived TGFβ1 Facilitates Blood-Brain Barrier Function via Non-Canonical Hedgehog Signaling in Brain Microvascular Endothelial Cells. Brain Sci 2021 Jan 8;11(1):77. PMID: 33430164
Inhibition of Wilms' Tumor Proliferation and Invasion by Blocking TGF- β Receptor I in the TGF- β/Smad Signaling Pathway. Biomed Res Int 2020 Nov 16:2020:8039840. PMID: 33282954
Induction of SPARC on Oxidative Stress, Inflammatory Phenotype Transformation, and Apoptosis of Human Brain Smooth Muscle Cells Via TGF-β1-NOX4 Pathway. J Mol Neurosci 2020 Nov;70(11):1728-1741. PMID: 32495004
Imbalance in the estrogen/androgen ratio may affect prostate fibrosis through the TGF-β/Smad signaling pathway. Int Urol Nephrol 2022 Mar;54(3):499-508. PMID: 35050457
Res Sq. 2026 Feb 2.
