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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-INCB059872
INCB059872

Chemical Structure : INCB059872

CAS No.: 1802909-49-4

INCB059872 (INCB-059872)

货号: PC-38127Not For Human Use, Lab Use Only.

INCB059872 (INCB-059872, INCB 59872) is a potent, selective, and orally active lysine-specific demethylase 1 (LSD1) inhibitor.

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

INCB059872 (INCB-059872, INCB 59872) is a potent, selective, and orally active lysine-specific demethylase 1 (LSD1) inhibitor.
INCB059872 inhibits the proliferation of a panel of SCLC cell lines with EC50 values ranging from 47 to 377 nM.
Oral administration of INCB059872 on once daily (QD) and alternative day (QoD) dosing regimens inhibited tumor growth in the NCI-H526 and NCI-H1417 human SCLC xenograft models.
INCB059872 treatment in these models led to the induction of the FEZ1 and UMODL1 genes relative to vehicle-treated animals, as part of a gene signature in SCLC cell lines that is predictive of LSD1 responsiveness.

物理化学性质&存储条件

分子量 386.536
分子式 C23H34N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 1 Month
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-((4-(methoxymethyl)-4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)cyclobutane-1-carboxylic acid

参考文献

1. Dai XJ, et al. J Med Chem. 2020 Dec 10;63(23):14197-14215.

2. Johnston G, et al. Gene. 2020 Aug 20;752:144758.

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