A DNA polymerase θ inhibitor
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RP 6685

Item No. 42127

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(6-amino-3-pyridazinyl)-2-propyn-1-yl]-N-(4-fluorophenyl)-3,5-bis(trifluoromethyl)-2-pyridineacetamide
CAS Number
2832047-80-8
Molecular Formula
C22H14F7N5O
Formula Weight
497.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(CC1=NC=C(C(F)(F)F)C=C1C(F)(F)F)N(CC#CC2=CC=C(N=N2)N)C3=CC=C(C=C3)F
InChi Code
InChI=1S/C22H14F7N5O/c23-14-3-6-16(7-4-14)34(9-1-2-15-5-8-19(30)33-32-15)20(35)11-18-17(22(27,28)29)10-13(12-31-18)21(24,25)26/h3-8,10,12H,9,11H2,(H2,30,33)
InChi Key
LHFFKHVGAKIDNO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $164

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    10 mg

    $291

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    25 mg

    $545

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    Cayman Chemical
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    Product Description

    RP 6685 is an inhibitor of DNA polymerase θ (IC50 = 0.55 nM).1 It is selective for DNA polymerase θ over DNA polymerase α, -ε, -γ, and -ν (IC50s = >100 µM for all). RP 6685 inhibits double-strand break repair in adeno-associated virus 1 (AAVS1) loci in HCT116 cells (IC50 = 0.5 µM) and the proliferation of HCT116 BRCA2-/- cells (IC50 = 0.32 µM). In vivo, RP 6685 (80 mg/kg) reduces tumor volume in an HCT116 BRCA2-/- mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bubenik, M., Mader, P., Mochirian, P., et al. Identification of RP-6685, an orally bioavailable compound that inhibits the DNA polymerase activity of Polθ. J. Med. Chem. 65(19), 13198-13215 (2022).