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. 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CB17 SCID/SCID female mice bearing subcutaneous IM-9 multiple myeloma tumorsDosage: 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. Form:Solid
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Teglarinad chloride
CAS number：432037-57-5 molecular formula：C30H43Cl2N5O8
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| Chinese alias | 氯化替格拉利奈 | ||
| English alias | PYRIDINIUM, 4-((((6-(4-CHLOROPHENOXY)HEXYL)IMINO)(CYANOAMINO)METHYL)AMINO)-1-(3-OXO-2,4,7,10,13,16-HEXAOXAHEPTADEC-1-YL)-, CHLORIDE (1:1) | Teglarinad chloride [USAN:INN] | MS-31058 | [4-[[N'-[6-(4-chlorophenoxy)hexyl]-N-cyanocarbamimidoyl]amino]pyridin-1 | ||
| CAS number | 432037-57-5 | molecular formula | C30H43Cl2N5O8 |
| molecular weight | 672.60 g/mol | Exact mass | ≥98% |
| PSA | 146.000 Ų | logp | - |
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