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VLX600

Cat. No. M11226
VLX600 Structure
Synonym:

1622945-04-3

Size Price Availability Quantity
10mg USD 90  USD90 In stock
25mg USD 180  USD180 In stock
50mg USD 305  USD305 In stock
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Quality Control & Documentation
Biological Activity

VLX600 is a novel inhibitor of iron-chelated oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and can show enhanced cytotoxicity in nutrient deficiency conditions. VLX600 showed selective cytotoxic activity against malignant cells and induced autophagy and had anticancer activity.

*The compound is unstable in solutions, freshly prepared is recommended

Chemical Information
Molecular Weight 317.36
Formula C17H15N7
CAS Number 327031-55-0
Form Solid
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Thomas L Ekstrom, et al. Mol Cancer Ther. VLX600 Disrupts Homologous Recombination and Synergizes with PARP Inhibitors and Cisplatin by Inhibiting Histone Lysine Demethylases

[2] Henning Karlsson, et al. Oncotarget. A novel tumor spheroid model identifies selective enhancement of radiation by an inhibitor of oxidative phosphorylation

[3] Kabir Mody, et al. Invest New Drugs. A phase I study of the safety and tolerability of VLX600, an Iron Chelator, in patients with refractory advanced solid tumors

[4] Gerardo A Vitiello, et al. Clin Cancer Res. Mitochondrial Inhibition Augments the Efficacy of Imatinib by Resetting the Metabolic Phenotype of Gastrointestinal Stromal Tumor

[5] Mrten Frykns, et al. Sci Rep. Iron chelators target both proliferating and quiescent cancer cells

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Keywords: VLX600, 1622945-04-3 supplier, Mitochondrial Related, inhibitors, activators


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