CBR-5884

Catalog No.S9645 Batch:S964501

Technical Data

Formula	C₁₄H₁₂N₂O₄S₂
Molecular Weight	336.39	CAS No.	681159-27-3
Solubility (25°C)*	In vitro	DMSO	67 mg/mL (199.17 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

CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity.

Targets

PHGDH ^[1]
(Cell-free assay)

33 μM

In vitro

CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. Biochemical characterization of the inhibitor reveals that it is a noncompetitive inhibitor that shows a time-dependent onset of inhibition and disrupts the oligomerization state of PHGDH.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Carney cells Concentrations 1 μM, 15 μM, 30 μM; 1 μM to 40 μM Incubation Time 1 h; 3 h Method Acute Toxicity Assay. Carney cells acclimated to growth in MEM media are plated in a 96-well plate at 6,000 cells per well. The next day, cells are treated with CBR-5884 from 1 μM to 40 μM for 3 h. Drug containing media are then removed, fresh drug-free media added, and cell viability is determined via a CellTiter-Glo or Alamar Blue assay according to the manufacturer’s protocol.

Cell Assay:^{^[1]}

Cell lines
Carney cells
Concentrations
1 μM, 15 μM, 30 μM; 1 μM to 40 μM
Incubation Time
1 h; 3 h
Method
Acute Toxicity Assay. Carney cells acclimated to growth in MEM media are plated in a 96-well plate at 6,000 cells per well. The next day, cells are treated with CBR-5884 from 1 μM to 40 μM for 3 h. Drug containing media are then removed, fresh drug-free media added, and cell viability is determined via a CellTiter-Glo or Alamar Blue assay according to the manufacturer’s protocol.

References

[1] Edouard Mullarky, et al. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.