For research use only. Not for therapeutic Use.
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[1]. 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.
RP-6685 is extremely potent with an IC50 of 550 pM against the pol activity of full-length Polθ and inactive on the ATPase activity[1].
RP-6685 inhibits Polθ in HEK293 LIG4-/- cellswith an IC50 of 0.94 μM[1].
RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice[1].
| Catalog Number | I042749 |
| CAS Number | 2832047-80-8 |
| Synonyms | N-[3-(6-aminopyridazin-3-yl)prop-2-ynyl]-2-[3,5-bis(trifluoromethyl)pyridin-2-yl]-N-(4-fluorophenyl)acetamide |
| Molecular Formula | C22H14F7N5O |
| Purity | ≥95% |
| InChI | 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) |
| InChIKey | LHFFKHVGAKIDNO-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC=C1N(CC#CC2=NN=C(C=C2)N)C(=O)CC3=C(C=C(C=N3)C(F)(F)F)C(F)(F)F)F |
| 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. |
