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Home - Products - Cell Cycle/DNA Damage - DNA/RNA Synthesis - RP-6685

RP-6685

CAS No. 2832047-80-8

RP-6685( —— )

Catalog No. M35367 CAS No. 2832047-80-8

RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    RP-6685
  • Note
    Research use only, not for human use.
  • Brief Description
    RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity.
  • Description
    RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model. RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Female CD1 nude mice (HCT116 BRCA2+/+ and BRCA2-/- xenograft tumor models)Dosage:80 mg/kg Administration:p.o.; BID for 21 days Result:Showed tumor regression during the first 8 days of treatment in BRCA2-/- HCT116 model, while did not inhibit tumor growth in BRCA2+/+ HCT116 tumors mice.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    DNA/RNA Synthesis
  • Recptor
    DNA/RNA Synthesis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2832047-80-8
  • Formula Weight
    497.37
  • Molecular Formula
    C22H14F7N5O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (201.06 mM; Ultrasonic )
  • SMILES
    Nc1ccc(nn1)C#CCN(C(=O)Cc1ncc(cc1C(F)(F)F)C(F)(F)F)c1ccc(F)cc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Bubenik M, et al. Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ. J Med Chem. 2022 Sep 20.?
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