产品
编 号：F428899
分子式：C20H21N3O2
分子量：335.4
分子式：C20H21N3O2
分子量：335.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
253
In-stock
5mg
558
In-stock
10mg
893
In-stock
50mg
2767
In-stock
结构图
CAS No: 694433-59-5
产品详情
生物活性：
SB-505124 is a selective inhibitor of?TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with?IC50s?of 129 nM and 47 nM for?ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
体内研究：
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.Animal Model:C57Bl6 mice with A549 xenografts
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.
体外研究：
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 IC50 value 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. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro. 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.
SB-505124 is a selective inhibitor of?TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with?IC50s?of 129 nM and 47 nM for?ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
体内研究：
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.Animal Model:C57Bl6 mice with A549 xenografts
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.
体外研究：
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 IC50 value 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. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro. 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.
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