SD-208

製品コードS7624 バッチS762404

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H10ClFN6
分子量 352.75 CAS No. 627536-09-8
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 17 mg/mL (48.19 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
in vitro 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] This compound 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] It also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro. [3]
in vivo SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. [1] In syngeneic 129S1 mice, this compound (60 mg/kg/d, p.o.) inhibits primary R3T tumor growth, and reduces the number and the size of lung metastases. [2] In the murine aortic allograft model, this chemical effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA). [3]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
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 this compound to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound.
細胞アッセイ 細胞株 Murine SMA-560 and human LN-308 glioma cells
濃度 1 μM
反応時間 48 hours
実験の流れ 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.
動物実験 動物モデル VM/Dk mice bearing SMA-560 tumors
投薬量 1 mg/mL
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15520202/
  • https://pubmed.ncbi.nlm.nih.gov/16857807/
  • https://pubmed.ncbi.nlm.nih.gov/24685405/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Nudifloside, a Secoiridoid Glucoside Derived from Callicarpa nudiflora, Inhibits Endothelial-to-Mesenchymal Transition and Angiogenesis in Endothelial Cells by Suppressing Ezrin Phosphorylation [ J Cancer, 2024, 15(9):2448-2459] PubMed: 38577590
Protein phosphatase PPM1A inhibition attenuates osteoarthritis via regulating TGF-β/Smad2 signaling in chondrocytes [ JCI Insight, 2023, 8(3)e166688] PubMed: 36752205
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 10.3390/cancers15205086] PubMed: 37894453
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 15(20)5086] PubMed: 37894453
Exosome-Mediated Delivery of Transforming Growth Factor-β Receptor 1 Kinase Inhibitors and Toll-Like Receptor 7/8 Agonists for Combination Therapy of Tumors [ Acta Biomater, 2022, S1742-7061(22)00004-6] PubMed: 35007784
Induction of Pro-Fibrotic CLIC4 in Dermal Fibroblasts by TGF-β/Wnt3a Is Mediated by GLI2 Upregulation [ Cells, 2022, 11(3)530] PubMed: 35159339
Berberine Suppresses Lung Metastasis of Cancer via Inhibiting Endothelial Transforming Growth Factor Beta Receptor 1 [ Front Pharmacol, 2022, 13:917827] PubMed: 35784732
TGFβ signaling is required for sclerotome resegmentation during development of the spinal column in Gallus gallus [ Dev Biol, 2022, 488:120-130] PubMed: 35644252
Loss of Yap/taz in cardiac fibroblasts attenuates adverse remodeling and improves cardiac function [ Cardiovasc Res, 2021, cvab205] PubMed: 34132780
Co-inhibition of SMAD and MAPK signaling enhances 124I uptake in BRAF-mutant thyroid cancers [ Endocr Relat Cancer, 2021, 28(6):391-402] PubMed: 33890869

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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