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GSK2879552 dihydrochloride
CAS No. 1902123-72-1
GSK2879552 dihydrochloride ( ——— )
产品货号. M38014 CAS No. 1902123-72-1
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
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生物学信息
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产品名称GSK2879552 dihydrochloride
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注意事项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
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产品简述GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
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产品描述GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
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体外实验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.
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体内实验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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同义词———
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通路Others
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靶点Other Targets
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受体KDM1/LSD1
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研究领域———
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适应症———
化学信息
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CAS Number1902123-72-1
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分子量437.4
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分子式C23H30Cl2N2O2
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纯度>98% (HPLC)
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溶解度H2O : 100 mg/mL (228.62 mM) DMSO : 31.25 mg/mL (71.44 mM)
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SMILES———
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化学全称———
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21.?
产品手册
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