GSK2879552 dihydrochloride

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

GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

GSK2879552 dihydrochloride (1.5 mg/kg，po) 处理在携带 SCLC 异种移植物的小鼠中表现出肿瘤生长抑制。Animal Model:NCI-H526 and NCI-H1417 xenografts.Dosage:1.5 mg/kg.Administration:PO daily for 25-35 days.Result:There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

GSK2879552 dihydrochloride 抑制 KDM1A 组蛋白去甲基化酶活性，诱导索拉非尼耐药细胞的分化并减弱干细胞特性。GSK2879552 dihydrochloride 在索拉非尼耐药细胞中抑制 Wnt 拮抗剂的转录并下调 β-catenin 信号活性。Cell Viability Assay.Cell Line:9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration:0-10000 nM.Incubation Time:6 days.Result:Inhibited cell proliferation.RT-PCR.Cell Line:Resistant HCC cells (PLC/PRF/5 and Huh7).Concentration:0, 1, 2 μM.Incubation Time:24 h.Result:Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

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Others

Other Targets

KDM1/LSD1

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1902123-72-1

437.4

C23H30Cl2N2O2

>98% (HPLC)

H2O : 100 mg/mL (228.62 mM) DMSO : 31.25 mg/mL (71.44 mM)

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(-20℃)

With Ice Pack

≥ 2 years