| Name | RP-6685 |
| Description | RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Polθ), manifests remarkable oral activity. With an IC 50 value of 5.8 nM in the PicoGreen assay, RP-6685 effectively hinders the enzymatic activity of Polθ. In addition, it demonstrates significant antitumor efficacy as observed in a mouse tumor xenograft model [1]. |
| In vitro | RP-6685 demonstrates high potency, with an IC50 of 550 pM against the pol activity of full-length Polθ and no effect on ATPase activity [1]. In HEK293 LIG4 -/- cells, RP-6685 inhibits Polθ with an IC50 of 0.94 μM [1]. |
| In vivo | Administering RP-6685 at a dosage of 80 mg/kg orally twice a day for 21 days demonstrated significant antitumor activity in BRCA2-deficient HCT116 mouse models. Despite inducing tumor regression within the first 8 days of treatment in BRCA2 -/- HCT116 models, it proved ineffective in BRCA2 +/+ HCT116 tumors. In another assessment using CD1 mice weighing 20-30 g, a single dose of either 2.5 mg/kg intravenously or orally was tested, yielding pharmacokinetic parameters of clearance (CL) at 36.8 mL/min/kg, a steady-state volume of distribution (V dss) at 1.1 L/kg, a half-life (t 1/2) of 0.4 hours, and a bioavailability (F) of 66%. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 3.3 mg/mL (6.63 mM), Sonication is recommended.
DMSO : 112.5 mg/mL (226.19 mM), Sonication is recommended.
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| Keywords | RP-6685 | RP6685 | RP 6685 | RNASynthesis | RNA Synthesis | DNASynthesis | DNA Synthesis | DNA polymerase |
| Inhibitors Related | 5-Fluorouracil | Adenine hemisulfate | Erythromycin thiocyanate | Guanidine hydrochloride | Hexane-1,6-diol | 1,4-Naphthoquinone | Adenine | Vidarabine | Carbazole | Thymidine | Docosanoic acid | Usnic Acid |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
