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SD-208
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SD-208图片
CAS NO:627536-09-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
SD208
ALK5 Inhibitor V
产品介绍
SD208 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。

产品描述

SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.

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)

Cas No.

627536-09-8

分子式

C17H10ClFN6

分子量

352.75

别名

SD208;ALK5 Inhibitor V

储存和溶解度

DMSO:7.1 mg/mL (20 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years