Teglarinad chloride

Modify Date: 2024-04-06 12:01:04

Teglarinad chloride Structure
Teglarinad chloride structure
Common Name Teglarinad chloride
CAS Number 432037-57-5 Molecular Weight 672.59700
Density N/A Boiling Point N/A
Molecular Formula C30H43Cl2N5O8 Melting Point 158-159ºC
MSDS N/A Flash Point N/A

 Use of Teglarinad chloride


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].

 Names

Name [4-[[N'-[6-(4-chlorophenoxy)hexyl]-N-cyanocarbamimidoyl]amino]pyridin-1-ium-1-yl]methyl 2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethyl carbonate,chloride
Synonym More Synonyms

 Teglarinad chloride Biological Activity

Description 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].
Related Catalog
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 75mg/kg. Reduced IM-9 tumor growth moderately At 37.5mg/kg.
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.

[2]. Beauparlant P, et, al. Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. 2009 Jun;20(5):346-54.

 Chemical & Physical Properties

Melting Point 158-159ºC
Molecular Formula C30H43Cl2N5O8
Molecular Weight 672.59700
Exact Mass 671.24900
PSA 147.15000
LogP 5.10808

 Safety Information

Hazard Codes Xi

 Synonyms

GMX1777
UNII-D6V5QYX9MZ
Teglarinad chloride