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ART558

Cat. No. M21168
ART558 Structure
Size Price Availability Quantity
5mg USD 480  USD480 In stock
10mg USD 820  USD820 In stock
25mg USD 1750  USD1750 In stock
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Quality Control & Documentation
Biological Activity

ART558 is a nanomolar, highly potent, selective, low-molecular-weight, variant DNA polymerase active Polθ inhibitor (IC50=7.9 nM). ART558 can be used in cancer research.

Chemical Information
Molecular Weight 418.41
Formula C21H21F3N4O2
CAS Number 2603528-97-6
Form Solid
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage 2-8°C, protect from light, dry, sealed
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] Joost Schimmel, et al. Cell Rep. Modulating mutational outcomes and improving precise gene editing at CRISPR-Cas9-induced breaks by chemical inhibition of end-joining pathways

[2] Gonzalo Rodriguez-Berriguete, et al. Clin Cancer Res. Small-molecule Polθ inhibitors provide safe and effective tumor radiosensitization in preclinical models

[3] Martin L Stockley, et al. J Med Chem. Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta

[4] Diana Zatreanu, et al. Nat Commun. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance

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Keywords: ART558 supplier, DNA/RNA Synthesis, inhibitors, activators


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