GMB-475

Catalog No.S8888 Batch:S888802

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Technical Data

Formula

C43H46F3N7O7S

Molecular Weight 861.93 CAS No. 2490599-18-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (116.01 mM)
Ethanol 100 mg/mL (116.01 mM)
Water 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.)

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Biological Activity

Description GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
Targets
BCR-ABL1 [1] E3 ligase [1]
In vitro

GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition, while demonstrating no toxicity toward Ba/F3 parental cells.[1]

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells)

  • Concentrations

    0.001-0.300 μM, 5 μM

  • Incubation Time

    3 days, 8 h

  • Method

    Cell viability assay: Cell lines and patient samples are exposed to dose ranges of GMB-475 (0.001-0.300 μM) and incubated for 3 days at 37°C, 5% CO2 and subjected to a CellTiter 96 AQueous One solution cell proliferation assay. Reverse phase protein arrays (RPPA): K562 cells are treated with DMSO, GMB-475 (5 μM) for 8 h in duplicate, washed twice with PBS and lysed in RPPA lysis buffer.

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.