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。
货号:ajcx32128
CAS:432037-57-5
分子式:C30H43Cl2N5O8
分子量：672.6
溶解度:DMSO: 200 mg/mL (297.35 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.