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Teglarinad chloride

Catalog No.GC61622

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.

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Teglarinad chloride Chemical Structure

Cas No.: 432037-57-5

Size Price Stock Qty
5 mg
$371.00
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10 mg
$630.00
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25 mg
$1,251.00
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50 mg
$2,039.00
In stock
100 mg
$3,152.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

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]

[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 Properties

Cas No. 432037-57-5 SDF
Canonical SMILES N#CN/C(NC1=CC=[N+](C=C1)COC(OCCOCCOCCOCCOC)=O)=N/CCCCCCOC2=CC=C(C=C2)Cl.[Cl-]
Formula C30H43Cl2N5O8 M.Wt 672.6
Solubility DMSO: 200 mg/mL (297.35 mM) Storage -20°C, away from moisture and light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.4868 mL 7.4338 mL 14.8677 mL
5 mM 0.2974 mL 1.4868 mL 2.9735 mL
10 mM 0.1487 mL 0.7434 mL 1.4868 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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