315702-40-0
中文名稱
化合物CEEFOURIN 1
英文名稱
Ceefourin 1
CAS
315702-40-0
分子式
C11H10N4S3
分子量
294.42
MOL 文件
315702-40-0.mol
315702-40-0 結(jié)構(gòu)式
基本信息
中文別名
化合物CEEFOURIN 1 英文別名
Ceefourin 15-[(2-Benzothiazolylthio)methyl]-2,4-dihydro-4-methyl-3H-1,2,4-triazole-3-thione
P-glycoprotein,chemosensitizers,inhibit,efflux,protein,resistance,Ceefourin 1,Ceefourin1,MRP4,HEK293,D-luciferin,ABC,ABCG2,P-gp,multidrug,MRP1,Inhibitor,neuroblastoma,Ceefourin-1,ABCC1,BCRP
物理化學(xué)性質(zhì)
熔點(diǎn)181° - 182°C
儲(chǔ)存條件-20°C, Inert atmosphere
溶解度氯仿（微溶）、甲醇（微溶、加熱）
形態(tài)固體
顏色淡黃色
常見問題列表
生物活性
Ceefourin 1 是一種有效且高度選擇性的多藥抗性蛋白 4 (MRP4) 抑制劑。Ceefourin 1 抑制多種 MRP4 底物的轉(zhuǎn)運(yùn)，但對(duì)其他 ABC 轉(zhuǎn)運(yùn)蛋白沒有選擇性。Ceefourin 1 是一種苯并噻唑，主要用作高危神經(jīng)母細(xì)胞瘤的化學(xué)增敏劑。靶點(diǎn)
MRP4
體外研究
Ceefourin 1 are highly selective for MRP4 over other ABC transporters, including P-glycoprotein (P-gp), ABCG2 (Breast Cancer Resistance Protein; BCRP) and MRP1 (ABCC1). Ceefourin 1 has limited off-target effects and high stability.
Ceefourin 1 (100 nM-100 μM) has low cellular toxicity (IC
50
>50) in two normal (HSF, MRC5), seven neuroblastoma (BE(2)-C, IMR-32, LAN-1, IMR-32, SK-N-SH, NBL-WN, SHEP) and four other human cancer cell lines (HEPG2, LNCap, SJ-G2, MCF7).
Ceefourin 1 has an IC
50
of 2.5 μM in HEK293 cell. Ceefourin 1 blocks D-luciferin efflux with an IC
50
of 1.5 μM.