GMX-1777 chloride

Research use only, not for human use.

A potent and specific inhibitor of the NAD(+) biosynthesis enzyme NAMPT with IC50 of <20 nM.

The water-soluble prodrug of GMX-1778 (CHS-828), which is a potent and specific inhibitor of the NAD(+) biosynthesis enzyme NAMPT with IC50 of <20 nM; shows anticancer activity in clinical trials, can be used in combination with other drugs to treat malignant melanoma.Blood Cancer Phase 1 Clinical.

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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.

GMX1777 chloride | Teglarinad | EB-1627

Metabolic Enzyme/Protease

NAMPT

NAMPT

Cancer

Blood cancer

432037-57-5

672.601

C30H43Cl2N5O8

>98% (HPLC)

100 mM in H2O

COCCOCCOCCOCCOC(=O)OC[N+]1=CC=C(C=C1)NC(=NCCCCCCOC2=CC=C(C=C2)Cl)NC#N.[Cl-]

[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

(-20℃)

With Ice Pack

≥ 2 years