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UPGL00004

🥰Excellent
Catalog No. T17206Cas No. 1890169-95-5

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.

UPGL00004

UPGL00004

🥰Excellent
Purity: 97.93%
Catalog No. T17206Cas No. 1890169-95-5
UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$46In StockIn Stock
25 mg$94In StockIn Stock
50 mg$163In StockIn Stock
100 mg$237In StockIn Stock
1 mL x 10 mM (in DMSO)$30In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:97.93%
Appearance:Solid
Color:Red
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Product Introduction

Bioactivity
Description
UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.
Targets&IC50
Glutaminase C:(kd)27 nM, Glutaminase C:29 nM, Glutaminase C:27 nM(kd), Glutaminase C:29 nM
In vitro
UPGL00004 inhibits MDA-MB-231, HS578T, and TSE cells (IC50s: 70, 129, and 262 nM, respectively).[1]
In vivo
In a triple-negative breast cancer patient-derived tumor graft model, the combination of UPGL00004 (1 mg/kg body weight) and Bevacizumab (2.5 mg/kg body weight) via intraperitoneal injection completely prevent any detectable increase in tumor size.[1]
Chemical Properties
Molecular Weight534.66
FormulaC25H26N8O2S2
Cas No.1890169-95-5
SmilesO=C(Cc1ccccc1)Nc1nnc(NC2CCN(CC2)c2nnc(NC(=O)Cc3ccccc3)s2)s1
Relative Density.1.460 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 112.5 mg/mL (210.41 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8703 mL9.3517 mL18.7035 mL93.5174 mL
5 mM0.3741 mL1.8703 mL3.7407 mL18.7035 mL
10 mM0.1870 mL0.9352 mL1.8703 mL9.3517 mL
20 mM0.0935 mL0.4676 mL0.9352 mL4.6759 mL
50 mM0.0374 mL0.1870 mL0.3741 mL1.8703 mL
100 mM0.0187 mL0.0935 mL0.1870 mL0.9352 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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