- 英文名称
- Zotiraciclib
- 分子式
- C23H24N4O
- 分子量
- 372.46
- 中文别名
- 14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯; TG-02; TG 02; TG02; SB1317; SB-1317; SB 1317; (E/Z)-Zotiraciclib; 6-Methyl-12-oxa-3,6-diaza-2(4,2)-pyrimidina-1,4(1,3)-dibenzenacyclododecaphan-8-ene; sb1317; (16E)-14-Methyl-20-oxa-5,7,14,27-tetraazatetracyclo[19.3.1.1.1]heptacosa-1(25),2(27),3,5,8(26),9,11,16,21,23-decaene; sb 1317; tg 02; sb-1317/tg02; TG-02/SB-1317; 14-Methyl-20-oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene; TG02; TG-02; 20-Oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 14-methyl-
- 用途
- 化学合成;作为有效的CDK2、JAK2和FLT3抑制剂;抑制HCT-116(IC50=0.079μm)和HL-60(IC50=0.059μm)细胞增殖;在体外主要由CYP3A4和CYP1A2代谢;对人CYP1A2、3A4、2C9和2C19亚型无抑制作用,但抑制CYP2D6(IC50=0.95μm);在体外对人肝细胞无明显诱导作用;以75mg/kg po q.d.3×/周剂量治疗可显著抑制肿瘤生长(平均TGI为82%);口服和IP给药方法的平均TGIS分别为42%和63%;在小鼠、大鼠和狗体内具有中到高系统清除率、高分布量(>0.6l/kg),口服生物利用度分别为24%、4%和37%