Teglarinad (chloride)


CAS No. : 432037-57-5

(Synonyms: GMX1777; EB-1627)

432037-57-5
Price and Availability of CAS No. : 432037-57-5
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Cat. No. : HY-10080
M.Wt: 672.60
Formula: C30H43Cl2N5O8
Purity: >98 %
Solubility: DMSO : 200 mg/mL (297.35 mM; Need ultrasonic)
Introduction of 432037-57-5 :

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]. 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].

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