2231079-74-4
中文名稱(chēng)
NCT-505
英文名稱(chēng)
NCT-505
CAS
2231079-74-4
分子式
C27H28FN5O3S
分子量
521.61
MOL 文件
2231079-74-4.mol
2231079-74-4 結(jié)構(gòu)式
基本信息
中文別名
化合物NCT-505 英文別名
NCT-505 free base1-(6-Fluoro-3-(4-(methylsulfonyl)piperazine-1-carbonyl)quinolin-4-yl)-4-phenylpiperidine-4-carbonitrile
4-Piperidinecarbonitrile, 1-[6-fluoro-3-[[4-(methylsulfonyl)-1-piperazinyl]carbonyl]-4-quinolinyl]-4-phenyl-
應(yīng)用領(lǐng)域
用途一
NCT-505 is an Orally Bioavailable aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitor with Potent Cellular Activity (IC50 = 7 nM). NCT-505 demonstrated target engagement in a cellular thermal shift assay (CETSA), inhibited the formation of 3D spheroid cultures of OV-90 cancer cells, and potentiated the cytotoxicity of paclitaxel in SKOV-3-TR, a paclitaxel resistant ovarian cancer cell line. NCT-505 also exhibit high specificity over other ALDH isozymes and unrelated dehydrogenases.常見(jiàn)問(wèn)題列表
概述
NCT-505 是一種有效的，選擇性的乙醛脫氫酶 (aldehyde dehydrogenase (ALDH1A1)) 抑制劑，IC50 值為 7 nM，對(duì) hALDH1A2，hALDH1A3，hALDH2，hALDH3A1 的抑制作用較弱，IC50 值分別為 >57，22.8，20.1，>57 μM。