UPGL00004

Catalog No.S8778

For research use only.

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.

UPGL00004 Chemical Structure

CAS No. 1890169-95-5

Purity & Quality Control

Choose Selective Glutaminase Inhibitors

Biological Activity

Description UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.
Targets
glutaminase C [1]
(Cell-free assay)
29 nM
In vitro

UPGL00004 potently inhibits the growth of triple negative breast cancer cells, as well as tumor growth when combined with the anti-VEGF antibody bevacizumab[2].

In vivo

UPGL00004 potently suppresses tumor growth in a patient-derived xenograft model for breast cancer, when combined with the anti-angiogenesis, anti-VEGF monoclonal antibody bevacizumab[2].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Breast cancer cells
  • Concentrations: 0-10 μM
  • Incubation Time: 6 days
  • Method:

    Breast cancer cells are maintained in complete media (RPMI 1640 supplemented with 10% FBS) at 37°C and in a 5% CO2 atmosphere. For assays, cells are distributed into the wells of a 12 well plate at a density of 1 × 104 cells per well. The cells are allowed to attach to the plate overnight, and then are treated for 6 days with the indicated amounts of each drug, or a DMSO control, in complete media. The media and drugs are refreshed every two days. On the sixth day, the cells are removed from the plates with trypsin, and counted manually with a hemocytometer.

Animal Research:

[2]

  • Animal Models: triple-negative breast cancer patient-derived tumor graft (PDX) model (NOD/SCID mice)
  • Dosages: 1 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 25 mg/mL
(46.75 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 534.66
Formula

C25H26N8O2S2

CAS No. 1890169-95-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1NC2=NN=C(S2)NC(=O)CC3=CC=CC=C3)C4=NN=C(S4)NC(=O)CC5=CC=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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