| Identification | Back Directory | [Name]
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 | [Synonyms]
Gmx1777
EB-1627
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 | [Molecular Formula]
C30H43Cl2N5O8 | [MDL Number]
MFCD16038864 | [MOL File]
432037-57-5.mol | [Molecular Weight]
672.597 |
| Hazard Information | Back Directory | [Uses]
Teglarinad chloride (GMX1777) is a proagent 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]. | [in vivo]
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] | | 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.
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| [References]
[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. DOI:10.1158/1078-0432.CCR-09-1945
[2] Beauparlant P, et, al. Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. 2009 Jun;20(5):346-54. DOI:10.1097/CAD.0b013e3283287c20 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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