RP-6685 (RP6685) | Polθ inhibitor | Probechem Biochemicals

Chemical Structure : RP-6685

CAS No.: 2832047-80-8

RP-6685 (RP6685, RP 6685)

Catalog No.: PC-49348Not For Human Use, Lab Use Only.

RP-6685 (RP6685) is a potent, selective and orally bioavailable inhibitor of DNA polymerase theta (Polθ) with IC50 of 5.8 nM in PicoGreen assay (0.3 nM Polθ enzyme).

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5 mg	$138	In stock
10 mg	$218	In stock
25 mg	$358	In stock
50 mg	$558	In stock
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Biological Activity

RP-6685 (RP6685) is a potent, selective and orally bioavailable inhibitor of DNA polymerase theta (Polθ) with IC50 of 5.8 nM in PicoGreen assay (0.3 nM Polθ enzyme).

RP-6685 displays no inhibition against Pols α, ε, γ, ν (IC50 values >100 uM).

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.

RP-6685 treated cells isolated from tumors showed a modest trend toward increased micronuclei and γH2AX, which are hallmarks of DNA damage.

RP-6685 treatment caused a dosedependent decrease in MMEJ-mediated DNA repair in treated HEK293 cells, RP-6685 exhibited a potency of 0.5 uM in DSB repair of AAVS1 loci.

RP-6685 (80 mg/kg) showed tumor regression in an HCT116 BRCA2−/− mouse tumor xenograft model.

Physicochemical Properties

M.Wt	497.377
Formula	C22H14F7N5O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3-(6-aminopyridazin-3-yl)prop-2-yn-1-yl)-2-(3,5-bis(trifluoromethyl)pyridin-2-yl)-N-(4-fluorophenyl)acetamide

References

1. Bubenik M, et al. J Med Chem. 2022 Oct 13;65(19):13198-13215.

RP-6685 (RP6685, RP 6685)

Biological Activity

Physicochemical Properties

References

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