UPGL00004

Catalog No.S8778 Batch:S877801

Technical Data

Formula	C₂₅H₂₆N₈O₂S₂
Molecular Weight	534.66	CAS No.	1890169-95-5
Solubility (25°C)*	In vitro	DMSO	25 mg/mL (46.75 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[2]}	Animal Models triple-negative breast cancer patient-derived tumor graft (PDX) model (NOD/SCID mice) Dosages 1 mg/kg Administration i.p.

Cell Assay:^{^[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 Study:^{^[2]}

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

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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