Teglarinad chloride |
| Catalog No.GC61622 |
테글라리나드 클로라이드(GMX1777)는 GMX1778(니코틴아미드 포스포리보실 트랜스퍼라제 억제제)의 전구약물입니다. 테글라리나드 클로라이드는 마우스에서 항종양 활성을 나타내며 NAMPT의 억제에 기인할 수 있습니다. Teglarinad chloride는 또한 DNA 복구 및 항혈관신생에 대한 간섭에 의해 매개되는 방사선 효능을 향상시킵니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 432037-57-5
Sample solution is provided at 25 µL, 10mM.
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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.
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