RP-6685

RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC 50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model In Vitro RP-6685 is extremely potent with an IC 50 of 550 pM against the pol activity of full-length Polθ and inactive on the ATPase activity. RP-6685 inhibits Polθ in HEK293 LIG4 -/- cellswith an IC 50 of 0.94 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Animal Model: CD1 mice (20-30 g) Dosage: 2.5 mg/kg Administration: i.v. or p.o.; single dosage Result: CL (mL/min/kg) V dss (L/kg) t 1/2 (h) F (%) 36.8 1.1 0.4 66 Form:Solid IC50& Target:IC 50 : 5.8 nM (Polθ)

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