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Teglarinad chloride

Catalog No. T26254   CAS 432037-57-5
Synonyms: GMX 1777 chloride, EB1627, GMX1777, GMX1777 chloride, GMX 1777, GMX-1777 chloride, EB-1627, EB-1627 chloride, EB1627 chloride

Teglarinad chloride (GMX-1777 chloride) is a potent inhibitor of NAMPT, the precursor of GMX1778.Teglarinad chloride has antitumor activity and acts by interfering with DNA repair and inhibiting angiogenesis.

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Teglarinad chloride Chemical Structure
Teglarinad chloride, CAS 432037-57-5
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Purity: 98.09%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Teglarinad chloride (GMX-1777 chloride) is a potent inhibitor of NAMPT, the precursor of GMX1778.Teglarinad chloride has antitumor activity and acts by interfering with DNA repair and inhibiting angiogenesis.
In vivo In the IM-9 model, small-cell lung cancer (SHP-77) model, and colon carcinoma (HCT-116) model, GMX1777 (75 mg/kg; 24 h intravenous infusion) induces tumor regression[2].For both FaDu and C666-1 tumors in vivo, GMX1777 (50-100 mg/kg/day, intramuscular for 5 days), with or without local tumor radiotherapy, proves to be effective[1].Upon intravenous infusion (25-400 mg/kg; 24 h), GMX1777 is rapidly converted to GMX1778 in the plasma of mice, with a half-life of GMX1777 less than 0.7 h[1].
Synonyms GMX 1777 chloride, EB1627, GMX1777, GMX1777 chloride, GMX 1777, GMX-1777 chloride, EB-1627, EB-1627 chloride, EB1627 chloride
Molecular Weight 672.6
Formula C30H43Cl2N5O8
CAS No. 432037-57-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Beauparlant P, et, al. Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. 2009 Jun;20(5):346-54. 2. 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. 3. Olesen UH, Petersen JG, Garten A, Kiess W, Yoshino J, Imai S, Christensen MK, Fristrup P, Thougaard AV, Björkling F, Jensen PB, Nielsen SJ, Sehested M. Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase. BMC Cancer. 2010 Dec 12;10:677. doi: 10.1186/1471-2407-10-677. PubMed PMID: 21144000; PubMed Central PMCID: PMC3019212. 4. Bi TQ, Che XM. Nampt/PBEF/visfatin and cancer. Cancer Biol Ther. 2010 Jul 15;10(2):119-25. doi: 10.4161/cbt.10.2.12581. Epub 2010 Jul 3. Review. PubMed PMID: 20647743.

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Keywords

Teglarinad chloride 432037-57-5 Metabolism NAMPT GMX 1777 chloride Teglarinad Chloride EB1627 GMX1777 GMX1777 chloride GMX 1777 GMX1777 Chloride GMX-1777 chloride EB-1627 GMX-1777 EB-1627 chloride GMX 1777 Chloride GMX-1777 Chloride EB 1627 EB1627 chloride inhibitor inhibit

 

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