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SD-208 (ALK5 Inhibitor V) 是 TGF-βRI (ALK5) 的选择性抑制剂(IC50:48 nM),对其选择性是对 TGF-βRII 的 100 多倍。
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SD-208 (ALK5 Inhibitor V) 是 TGF-βRI (ALK5) 的选择性抑制剂(IC50:48 nM),对其选择性是对 TGF-βRII 的 100 多倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 108 | 现货 | |
2 mg | ¥ 148 | 现货 | |
5 mg | ¥ 235 | 现货 | |
10 mg | ¥ 380 | 现货 | |
25 mg | ¥ 768 | 现货 | |
50 mg | ¥ 1,180 | 现货 | |
100 mg | ¥ 1,780 | 现货 | |
200 mg | ¥ 2,630 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 417 | 现货 |
产品描述 | SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII. |
靶点活性 | TGFβRI:48 nM |
体外活性 | SD-208(1 mg/mL,p.o.)使负荷SMA-560胶质瘤小鼠的中值存活率显著延长.在同源129S1小鼠体内,SD-208(60 mg/kg,p.o.)抑制初级R3T肿瘤生长,并使肺转移的数量及大小减少.在小鼠大动脉同种移植模型中,SD-208可有效减少移植动脉硬化内膜增生的形成. |
体内活性 | 在体外,SD-208阻断TGF-β诱导的受体相关Smads,Smad/3磷酸化,且对上皮细胞到间叶细胞的分化转化、迁移及侵袭到基底膜具有刺激作用。在体外,SD-208还可阻断TGF-β对新生内膜平滑肌样细胞迁移与增殖的保护作用。在小鼠SMA-560和人SMA-560胶质瘤细胞中,SD-208抑制细胞生长、组成及转化生长因子-β诱发的迁移和浸润,并使免疫原性增强。 |
激酶实验 | 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 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. |
细胞实验 | 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.(Only for Reference) |
别名 | ALK5 Inhibitor V, SD208 |
分子量 | 352.75 |
分子式 | C17H10ClFN6 |
CAS No. | 627536-09-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 7.1 mg/mL (20 mM), Heating is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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