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SB-505124 hydrochloride
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。
SB-505124 hydrochloride图片
CAS NO:356559-13-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
SB-505124 hydrochloride 是一种选择性的 TGF-β Receptor type I receptor(ALK4ALK5ALK7) 抑制剂,对 LK4,ALK5 的 IC50值分别为 129 nM 和 47 nM,对 ALK1,2,3 或 6 无作用。
生物活性

SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptortype I receptor(ALK4,ALK5,ALK7), with IC50s of 129 nM and 47 nM for ALK4,ALK5, respectively, but it does not inhibitALK1, 2, 3, or 6.

IC50& Target

IC50: 129 nM (ALK4), 47 nM (ALK5)

体外研究
(In Vitro)

SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[3].

体内研究
(In Vivo)

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals[4].

Animal Model:C57Bl6 mice with A549 xenografts[4]
Dosage:5 mg/kg
Administration:I.p.; daily
Result:Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.
分子量

371.86

Formula

C20H22ClN3O2

CAS 号

356559-13-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.