RP-6685

SKU: orb1689787

Description

RP-6685 is a potent, selective, and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 of 5.8 nM. It demonstrates robust antitumor activity in mouse xenograft models, making it a valuable tool for investigating Polθ's role in DNA repair and oncology research, both in vitro and in vivo.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 2832047-80-8
• MW: 497.37
• Purity: 98.34% (May vary between batches)
• Formula: C₂₂H₁₄F₇N₅O
• SMILES: Nc1ccc(nn1)C#CCN(C(=O)Cc1ncc(cc1C(F)(F)F)C(F)(F)F)c1ccc(F)cc1
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (6.63 mM);DMSO:112.5 mg/mL (226.19 mM)

Bioactivity

• In Vivo:
  Administering RP-6685 at a dosage of 80 mg/kg orally twice a day for 21 days demonstrated significant antitumor activity in BRCA2-deficient HCT116 mouse models. Despite inducing tumor regression within the first 8 days of treatment in BRCA2 -/- HCT116 models, it proved ineffective in BRCA2 +/+ HCT116 tumors. In another assessment using CD1 mice weighing 20-30 g, a single dose of either 2.5 mg/kg intravenously or orally was tested, yielding pharmacokinetic parameters of clearance (CL) at 36.8 mL/min/kg, a steady-state volume of distribution (V dss) at 1.1 L/kg, a half-life (t 1/2) of 0.4 hours, and a bioavailability (F) of 66%.
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• In Vitro:
  RP-6685 demonstrates high potency, with an IC50 of 550 pM against the pol activity of full-length Polθ and no effect on ATPase activity . In HEK293 LIG4 -/- cells, RP-6685 inhibits Polθ with an IC50 of 0.94 μM .
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Storage & Handling

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

Alternative Names

RP 6685, RP6685, RP-6685, RNA Synthesis, RNASynthesis, DNASynthesis, DNA polymerase, DNA Synthesis

Compound Identifiers

PubChem CID

165413021