Teglarinad chloride (Synonyms: GMX1777; EB-1627)

Name: Teglarinad chloride
Brand: MedChemExpress
SKU: HY-10080
Rating: 4.5 (1 reviews)

Cat. No.: HY-10080 Purity: 98.77%: FAQs
Data Sheet SDS COA Handling Instructions

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Teglarinad chloride (GMX1777) is a proagent 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.

For research use only. We do not sell to patients.

Teglarinad chloride Chemical Structure

CAS No. : 432037-57-5

Size	Price	Stock	Quantity
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3400	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 75 mg/kg. Reduced IM-9 tumor growth moderately at 37.5 mg/kg.

Clinical Trial

Molecular Weight

672.60

Formula

C₃₀H₄₃Cl₂N₅O₈

CAS No.

432037-57-5

Appearance

Solid

Color

White to off-white

SMILES

N#CN/C(NC1=CC=[N+](C=C1)COC(OCCOCCOCCOCCOC)=O)=N/CCCCCCOC2=CC=C(C=C2)Cl.[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 66.67 mg/mL (99.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (7.43 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.77%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (245 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4868 mL	7.4338 mL	14.8677 mL	37.1692 mL
	5 mM	0.2974 mL	1.4868 mL	2.9735 mL	7.4338 mL
	10 mM	0.1487 mL	0.7434 mL	1.4868 mL	3.7169 mL
	15 mM	0.0991 mL	0.4956 mL	0.9912 mL	2.4779 mL
	20 mM	0.0743 mL	0.3717 mL	0.7434 mL	1.8585 mL
	25 mM	0.0595 mL	0.2974 mL	0.5947 mL	1.4868 mL
	30 mM	0.0496 mL	0.2478 mL	0.4956 mL	1.2390 mL
	40 mM	0.0372 mL	0.1858 mL	0.3717 mL	0.9292 mL
	50 mM	0.0297 mL	0.1487 mL	0.2974 mL	0.7434 mL
	60 mM	0.0248 mL	0.1239 mL	0.2478 mL	0.6195 mL
	80 mM	0.0186 mL	0.0929 mL	0.1858 mL	0.4646 mL

Teglarinad chloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Teglarinad chloride (Synonyms: GMX1777; EB-1627)

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Complete Stock Solution Preparation Table

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