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GSK-2879552
CAS No. 1401966-69-5
GSK-2879552 ( GSK2879552 )
产品货号. M11677 CAS No. 1401966-69-5
一种有效的、选择性不可逆的 LSD1 抑制剂，Ki app 为 1.7 uM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥381 | 有现货 |
|
| 5MG | ￥591 | 有现货 |
|
| 10MG | ￥948 | 有现货 |
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| 25MG | ￥1652 | 有现货 |
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| 50MG | ￥2989 | 有现货 |
|
| 100MG | ￥5613 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称GSK-2879552
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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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产品简述一种有效的、选择性不可逆的 LSD1 抑制剂，Ki app 为 1.7 uM。
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产品描述A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM; shows good selectivity against LSD2, MAO-A, MAO-B, D-amino acid oxidase and LoxL2; exhibits growth inhibition (EC50=2-240 nM) in sensitive cell lines; orally bioavailable.Lung Cancer Phase 1 Clinical.
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体外实验Cell Proliferation 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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体内实验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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同义词GSK2879552
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通路Chromatin/Epigenetic
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靶点Histone Demethylase
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受体LSD1
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研究领域Cancer
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适应症Lung Cancer
化学信息
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CAS Number1401966-69-5
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分子量364.4806
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分子式C23H28N2O2
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESO=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1
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化学全称Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-
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. Mohammad HP, et al. Cancer Cell. 2015 Jul 13;28(1):57-69.
2. Huang M, et al. Cancer Lett. 2017 Jul 10;398:12-21.
3. Maes T, et al. Epigenomics. 2015;7(4):609-26.
