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ART812

Cat. No. M21558
ART812  Structure
Size Price Availability
5mg USD 1035  USD1035 Custom Synthesis
10mg USD 1680  USD1680 Custom Synthesis
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Quality Control & Documentation
Biological Activity

ART812 is an orally effective DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 had an IC50 value of 240 nM for cell-based microhomologous mediated end-junction (MMEJ).

Chemical Information
Molecular Weight 461.79
Formula C19H16ClF4N3O4
CAS Number 2607138-82-7
Solubility (25°C) N/A
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] Gabriela Barszczewska-Pietraszek, et al. Int J Mol Sci. Polθ Inhibition: An Anticancer Therapy for HR-Deficient Tumours

[2] 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

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Keywords: ART812 supplier, DNA/RNA Synthesis, inhibitors, activators

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