| 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 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 112.5 mg/mL (226.2 mM), Sonication is recommended.
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| Keywords | RP-6685 | RP 6685 | RP6685 |
| Inhibitors Related | Rifampicin | 5-Fluorouracil | Ribavirin | Guanidine hydrochloride | 2,4-D | Resveratrol | Trimethoprim | Azelaic acid | Acyclovir | Thymidine | Temozolomide | Folic acid |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
