1257628-77-5

• 常用中文名：4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-b]吡啶-5-基)乙炔基]苯甲酰胺
• 常用英文名：GZD824
• CAS号：1257628-77-5
• 分子式：C₂₉H₂₇F₃N₆O
• 分子量：532.560
• 相关类别： 生物化工 抑制剂 蛋白酪氨酸激酶
• 发布时间：2016-08-18 21:54:39
• 更新时间：2026-07-10 16:10:28
• GZD824是新型口服的Bcr-Abl野生型和T315I突变型抑制剂,IC50分别为0.34和0.68nM。

名称

• 中文名: 4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-b]吡啶-5-基)乙炔基]苯甲酰胺
• 英文名: 3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
• 中文别名: GZ4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-B]吡啶-5-基)乙炔基]苯甲酰胺; BCR-ABL野生型和T315I突变型抑制剂(GZD824); 奥瑞巴替尼布; 抑制剂GZD824; 奥雷巴替尼; 3-[(1H-吡唑并[3,4-B]吡啶-5-基)乙炔基]-4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]苯甲酰胺; 耐克替尼; 3-((1H-吡唑并[3,4-B]吡啶-5-基)乙炔基)-4-甲基-N(4-((4-甲基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)苯甲酰胺; 4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-B]吡啶-5-基)乙炔基]苯甲酰胺
• 英文别名: Olverembatinib; 3-[(1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide; GZD-824 Free; 4-Methyl-N-{4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-3-(1H-pyrazolo[3,4-b]pyridin-5-ylethynyl)benzamide; 4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-3-(2-{1H-pyrazolo[3,4-b]pyridin-5-yl}ethynyl)benzamide; Olverembatinib, 10 mM in DMSO; GZD 824 //BP; Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]; GZD-824; GZD 824;BENZAMIDE; GZD8824; 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide; GZD824;GZD-824;GZD; 4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamide; GZD-824; Olverembatinib (GZD824)

物化性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 630.4±55.0 °C at 760 mmHg
• 分子式: C₂₉H₂₇F₃N₆O
• 分子量: 532.560
• 闪点: 335.0±31.5 °C
• 精确质量: 532.219849
• PSA: 77.15000
• LogP: 3.93
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.667
• 储存条件: -20°C

生物活性

• 描述: GZD824是新型口服的Bcr-Abl野生型和T315I突变型抑制剂,IC50分别为0.34和0.68nM。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL
  研究领域 >> 癌症
• 参考文献:

  [1]. Ren X, Pan X, Zhang Z, Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against

合成路线

1207351-08-3 ~% 1257628-77-5

文献：Ren, Xiaomei; Pan, Xiaofen; Zhang, Zhang; Wang, Deping; Lu, Xiaoyun; Li, Yupeng; Wen, Donghai; Long, Huoyou; Luo, Jinfeng; Feng, Yubing; Zhuang, Xiaoxi; Zhang, Fengxiang; Liu, Jianqi; Leng, Fang; Lang, Xingfen; Bai, Yang; She, Miaoqin; Tu, Zhengchao; Pan, Jingxuan; Ding, Ke Journal of Medicinal Chemistry, 2013 ,  vol. 56,  # 3  p. 879 - 894

上下游产品

上游产品  1
1207351-08-3
下游产品  0