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RP-6685

Catalog No. T60187 CAS 2832047-80-8

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].

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RP-6685, CAS 2832047-80-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 198.00
5 mg	In stock	$ 513.00
10 mg	In stock	$ 747.00
25 mg	In stock	$ 1,160.00
50 mg	In stock	$ 1,560.00
100 mg	In stock	$ 2,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 562.00

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Purity: 98.34%

Biological Description

Chemical Properties

Storage & Solubility Information

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 is extremely potent with an IC 50 of 550 pM against the pol activity of full-length Polθ whereas inactive on the ATPase activity [1]. RP-6685 inhibits Polθ in HEK293 LIG4 -/- cellswith an IC 50 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%.

Molecular Weight	497.37
Formula	C22H14F7N5O
CAS No.	2832047-80-8

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 112.5 mg/mL (226.2 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library DNA Damage & Repair Compound Library Bioactive Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RP-6685 2832047-80-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis RP 6685 RP6685 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.