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编 号:F357090
分子式:C30H43Cl2N5O8
分子量:672.6
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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.
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