SB-505124

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB505124 是 ALK4、ALK5 的 TGFβR 选择性抑制剂，无细胞测定中的 IC50 分别为 129 nM 和 47 nM，也抑制 ALK7，但不抑制 ALK1、2、3 或 6。

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.

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 (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.

SB505124 | SB-505124 | SB 505124

Angiogenesis

ALK

ALK4| ALK5

Cancer

——

694433-59-5

335.4

C20H21N3O2

>98% (HPLC)

Ethanol: 67 mg/mL (199.76 mM); DMSO: 67 mg/mL (199.76 mM)

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1

2-(4-(benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl)-6-methylpyridine

(-20℃)

With Ice Pack

≥ 2 years