432037-57-5
中文名稱
1-[[[[2-[2-[2-[2-甲氧基乙氧基]乙氧基]乙氧基]乙氧基]羰基]氧基]甲基]-4-[N'-氰基-N''-[6-[4-氯苯氧基]己基]胍基]氯化吡啶
英文名稱
1-[[[[2-[2-[2-[2-Methoxyethoxy]ethoxy]ethoxy]ethoxy]carbonyl]oxy]methyl]-4-[N'-cyano-N''-[6-[4-chlorophenoxy]hexyl]guanidino]pyridinium chloride
CAS
432037-57-5
分子式
C30H43ClN5O8.Cl
分子量
672.61
MOL 文件
432037-57-5.mol
432037-57-5 結(jié)構(gòu)式
基本信息
中文別名
1-[[[[2-[2-[2-[2-甲氧基乙氧基]乙氧基]乙氧基]乙氧基]羰基]氧基]甲基]-4-[N'-氰基-N''-[6-[4-氯苯氧基]己基]胍基]氯化吡啶 英文別名
EB-1627Gmx1777
Gmx 1777
Teglarinad
Teglarinad chloride
GMX1777
GMX 1777
GMX-1777
DAHMXVAETAAQOZ-UHFFFAOYSA-N
1-[[[[2-[2-[2-[2-Methoxyethoxy]ethoxy]ethoxy]ethoxy]carbonyl]oxy]methyl]-4-[N'-cyano-N''-[6-[4-chlorophenoxy]hexyl]guanidino]pyridinium chloride
1-[[[[2-[2-[2-[2-Methoxyethoxy]ethoxy]ethoxy]ethoxy]carbonyl]oxy]methyl]-4-[N'-cyano-N''-[6-[4-chlorophenoxy]hexyl]guanidino]pyridinium chloride ISO 9001：2015 REACH
所屬類別
醫(yī)藥中間體：氰基吡啶常見問題列表
生物活性
Teglarinad chloride (GMX1777) 是 GMX1778 (一種煙酰胺磷酸核糖基轉(zhuǎn)移酶抑制劑) 的前藥。Teglarinad chloride 在小鼠中表現(xiàn)出抗腫瘤活性可以歸因于 NAMPT 的抑制。Teglarinad chloride 通過干擾 DNA 修復(fù)和抗血管生成，可以增強(qiáng)放射功效。體內(nèi)研究
GMX1777 (75 mg/kg; 24 h intravenous infusion) causes tumor regression in the IM-9 model, a small-cell lung cancer (SHP-77) model, and a colon carcinoma (HCT-116) model.
GMX1777 (50-100 mg/kg/d, i.m. for 5 d) with or without local tumor radiotherapy is effective for both FaDu and C666-1 tumors in vivo.
GMX1777 (25-400 mg/kg; 24 h intravenous infusion) is quickly converted to GMX1778 in plasma of mice with a half-life of GMX1777 less than 0.7 h.
| Animal Model: | CB17 SCID/SCID female mice bearing subcutaneous IM-9 multiple myeloma tumors |
| Dosage: | 18.75, 35, 75 mg/kg |
| Administration: | A 24 h intravenous infusion |
| Result: |
Induced a nearly complete regression of the tumors and a significant tumor growth delay at the dose of 75 mg/kg.
Reduced IM-9 tumor growth moderately at 37.5 mg/kg. |