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Teglarinad chloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Teglarinad chloride图片
CAS NO:432037-57-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Teglarinadchloride(GMX1777)是GMX1778(一种烟酰胺磷酸核糖基转移酶抑制剂)的前药。Teglarinadchloride在小鼠中表现出抗肿瘤活性可以归因于NAMPT的抑制。Teglarinadchloride通过干扰DNA修复和抗血管生成,可以增强放射功效。
Cas No.432037-57-5
别名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,GMX1777; EB-1627
Canonical SMILESN#CN/C(NC1=CC=[N+](C=C1)COC(OCCOCCOCCOCCOC)=O)=N/CCCCCCOC2=CC=C(C=C2)Cl.[Cl-]
分子式C30H43Cl2N5O8
分子量672.6
溶解度DMSO: 200 mg/mL (297.35 mM)
储存条件-20℃, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis[1][2].

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[2].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[1].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[2]. Animal Model: CB17 SCID/SCID female mice bearing subcutaneous IM-9 multiple myeloma tumors[2]

[1]. Kato H, et, al. Efficacy of combining GMX1777 with radiation therapy for human head and neck carcinoma. Clin Cancer Res. 2010 Feb 1;16(3):898-911. [2]. Beauparlant P, et, al. Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. 2009 Jun;20(5):346-54.