ART812

SKU: orb1690736

Description

ART812 is a potent, orally bioavailable small molecule inhibitor of DNA polymerase theta (Polθ), with an enzymatic IC50 of 7.6 nM and a cellular MMEJ inhibition IC50 of 240 nM. This inhibitor is a valuable research tool for studying DNA repair pathways, particularly in the context of cancer research, where Polθ is a promising therapeutic target.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 2607138-82-7
• MW: 461.79
• Purity: 99.07% (May vary between batches)
• Formula: C₁₉H₁₆ClF₄N₃O₄
• SMILES: CN(C(=O)[C@@H]1[C@H](O)[C@H](O)C(=O)N1c1cc(cc(C)n1)C(F)(F)F)c1ccc(F)c(Cl)c1
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.15 mM);DMSO:90 mg/mL (194.89 mM)

Bioactivity

• Target IC50:
  Polymerase θ:7.6 nM (IC50)
• In Vivo:
  ART812 (100 mg/kg; p.o. daily for 76 days) shows significant tumour inhibition in rats bearing established MDA-MB-436 BRCA1/SHLD2 defective tumours (volume 250-350 mm 3 ) .
  Read more...
• In Vitro:
  ART812 (0-40 μM) induces Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells .

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNASynthesis, DNA polymerase θ, DNA Synthesis, ART812, ART-812, ART 812, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

156077039