SD-208
Based on 10 publication(s) in Google Scholar
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.44%
- CAS 番号: 627536-09-8
- 分子式: C17H10ClFN6
- 分子量:352.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 SD-208
More- Cell Death Dis. 2024 Dec 24;15(12):930. [Abstract]
- Cell Rep. 2020 Apr.
- FEBS J. 2026 Feb 2. [Abstract]
- J Clin Transl Hepatol. 2023 Feb 28;11(1):1-14. [Abstract]
- Cell Biol Int. 2020 Mar;44(3):861-872. [Abstract]
- Brain Sci. 2021 Jan 8;11(1):77. [Abstract]
- J Mol Neurosci. 2020 Nov;70(11):1728-1741. [Abstract]
- Biomed Res Int. 2020 Nov 16;2020:8039840. [Abstract]
- Int Urol Nephrol. 2022 Mar;54(3):499-508. [Abstract]
- Res Sq. 2026 Feb 2.
Customer Validation & Images
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WB
生物活性
IC50: 48 nM (TGF-βRI)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>25 μM
Compound: 1, SCI-208
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Cytotoxicity against Huh7 cells by luciferase assay
Cytotoxicity against Huh7 cells by luciferase assay
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[PMID: 17289388] |
| MT4 | CC50 |
>25 μM
Compound: 1, SCI-208
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Cytotoxicity against MT4 cells by luciferase assay
Cytotoxicity against MT4 cells by luciferase assay
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[PMID: 17289388] |
SD-208 inhibits the cell growth and constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity in murine SMA-560 and human LN-308 glioma cells[1]. SD-208 blocks TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro[2]. SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 627536-09-8
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性状 Solid
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分子量 352.75
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分子式 C17H10ClFN6
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Color Light yellow to yellow
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SMILES
FC1=CC=C(Cl)C=C1C2=NC3=NC=CN=C3C(NC4=CC=NC=C4)=N2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Ovarian cancer-derived TGF-β1 induces cancer-associated adipocytes formation by activating SMAD3/TRIB3 pathway to establish pre-metastatic niche. [Abstract]2024 Dec 24;15(12):930. PMID: 39719444 -
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FEBS J
Nemo-like kinase modulates glucocorticoid-induced erythroid progenitor differentiation by regulating stability of the glucocorticoid receptor. [Abstract]2026 Feb 2. PMID: 41629744 -
J Clin Transl Hepatol
Upregulation of GLT25D1 in Hepatic Stellate Cells Promotes Liver Fibrosis via the TGF-β1/SMAD3 Pathway In Vivo and In vitro. [Abstract]2023 Feb 28;11(1):1-14. PMID: 36406310 -
Cell Biol Int
TGF-β1 sustains germ cell cyst reservoir via restraining follicle formation in the chicken. [Abstract]2020 Mar;44(3):861-872. PMID: 31825139 -
Brain Sci
Astrocyte-Derived TGFβ1 Facilitates Blood-Brain Barrier Function via Non-Canonical Hedgehog Signaling in Brain Microvascular Endothelial Cells. [Abstract]2021 Jan 8;11(1):77. PMID: 33430164
SD-208 purchased from MedChemExpress. Usage Cited in: Brain Sci. 2021 Jan 8;11(1):77. [Abstract]
The effects of SD208 injection (4 mg/kg i.v.) on the expression of ZO-1, Gli1 and Gli2 in mouse brains.
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J Mol Neurosci
Induction of SPARC on Oxidative Stress, Inflammatory Phenotype Transformation, and Apoptosis of Human Brain Smooth Muscle Cells Via TGF-β1-NOX4 Pathway. [Abstract]2020 Nov;70(11):1728-1741. PMID: 32495004 -
Biomed Res Int
Inhibition of Wilms' Tumor Proliferation and Invasion by Blocking TGF- β Receptor I in the TGF- β/Smad Signaling Pathway. [Abstract]2020 Nov 16;2020:8039840. PMID: 33282954 -
Int Urol Nephrol
Imbalance in the estrogen/androgen ratio may affect prostate fibrosis through the TGF-β/Smad signaling pathway. [Abstract]2022 Mar;54(3):499-508. PMID: 35050457 -
溶剤 & 溶解度
DMSO : 9.09 mg/mL (25.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.91 mg/mL (2.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.91 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.91 mg/mL (2.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.91 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (14.17 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
VM/Dk mice are purchased from the TSE Resource Center. Mice of 6 to 12 weeks of age are used for the survival experiments. Groups of eight mice are anesthesized before all intracranial procedures and placed in a stereotaxic fixation device. A burr hole is drilled in the skull 2 mm lateral to the bregma. The needle of a Hamilton syringe is introduced to a depth of 3 mm. SMA-560 cells [5×103cells] resuspended in a volume of 2 μL of PBS are injected into the right striatum. Three days later, the mice are allowed to drink SD-208 at 1 mg/mL in deionized water. The mice are observed daily and, in the survival experiments, sacrificed on development of neurologic symptoms.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8349 mL | 14.1743 mL | 28.3487 mL | 70.8717 mL |
| 5 mM | 0.5670 mL | 2.8349 mL | 5.6697 mL | 14.1743 mL | |
| 10 mM | 0.2835 mL | 1.4174 mL | 2.8349 mL | 7.0872 mL | |
| 15 mM | 0.1890 mL | 0.9450 mL | 1.8899 mL | 4.7248 mL | |
| 20 mM | 0.1417 mL | 0.7087 mL | 1.4174 mL | 3.5436 mL | |
| 25 mM | 0.1134 mL | 0.5670 mL | 1.1339 mL | 2.8349 mL |
SD-208 関連分類
HY-13227 関連分類
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