VLX600

Catalog No.S8943 Batch:S894301

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Technical Data

Formula

C17H15N7
Molecular Weight 317.35 CAS No. 327031-55-0
Solubility (25°C)* In vitro DMSO 13 mg/mL (40.96 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumour spheroids in a synergistic manner. This compound shows enhanced cytotoxic activity under conditions of nutrient starvation. It induces autophagy and mitochondrial inhibition with antitumour activity.
Targets
OXPHOS
In vitro

VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. Mitochondrial inhibition with this compound has a direct antitumour effect in vitro while appearing to promote glycolysis through increased AKT signalling and glucose transporter expression. When combined with imatinib, this chemical prevents imatinib-induced cell cycle escape and reduces p27 expression, leading to increased apoptosis when compared to imatinib alone.
In Vivo

VLX600 induces the formation of autolysosomes in vivo. This compound displays tumour growth inhibition in vivo. When combined with imatinib, it reduces p27 expression in vivo, and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoural effects of Kit inhibition.

Protocol (from reference)

Cell Assay:

[3]
  • Cell Lines

    human GIST-T1 cell line, human HG129 cell line, human GIST-882 cell line,

  • Concentrations

    2 μM, 6 μM, 12 μM

  • Incubation Time

    48–72h

  • Method

    To measure cell viability, 1 × 104 GIST-T1, GIST-882, and HG129 cells are seeded in replicates of 5 in a 96-well flat-bottomed plate (Falcon) and cultured for 48–72h with VLX600 or DMSO-only solvent controls.
Animal Study:

[1]
  • Animal Models

    female NMRI nu/nu mice (8–10 weeks old)

  • Dosages

    16 mg/kg

  • Administration

    IV

References

  • https://pubmed.ncbi.nlm.nih.gov/24548894/
  • https://pubmed.ncbi.nlm.nih.gov/31523395/
  • https://pubmed.ncbi.nlm.nih.gov/29246941/

Sellecks VLX600 Has Been Cited by 1 Publication

Iron Chelator VLX600 Inhibits Mitochondrial Respiration and Promotes Sensitization of Neuroblastoma Cells in Nutrition-Restricted Conditions [ Cancers (Basel), 2022, 14(13)3225] PubMed: 35805002

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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.