RP-6685
Based on 4 publication(s) in Google Scholar
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model. RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity : 99.88%
- CAS No.: 2832047-80-8
- Formula: C22H14F7N5O
- Molecular Weight:497.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RP-6685
MoreAll DNA/RNA Synthesis Isoforms
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Biological Activity
Description
IC50 & Target
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DNA Polymerase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>15 μM
Compound: RP-6685
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Antiproliferative activity against BRCA2 knock in human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days with media replacement for every 3 or 4 days
Antiproliferative activity against BRCA2 knock in human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days with media replacement for every 3 or 4 days
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[PMID: 36126059] |
| HCT-116 | IC50 |
0.32 μM
Compound: RP-6685
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Antiproliferative activity against BRCA2 knock out human HCT-116 cells assessed as inhibition of cell growth incubated for 12 to 14 days with media replacement for every 3 or 4 days
Antiproliferative activity against BRCA2 knock out human HCT-116 cells assessed as inhibition of cell growth incubated for 12 to 14 days with media replacement for every 3 or 4 days
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[PMID: 36126059] |
| HCT-116 | IC50 |
0.45 μM
Compound: RP-6685
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Inhibition of MMEJ-mediated DNA repair in CRSIPRR/Cas9-induced wildtype human HCT-116 cells incubated for 24 hrs by PCR analysis
Inhibition of MMEJ-mediated DNA repair in CRSIPRR/Cas9-induced wildtype human HCT-116 cells incubated for 24 hrs by PCR analysis
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[PMID: 36126059] |
| HEK-293T | IC50 |
2.147 x 10-6 M
Compound: RP-6685
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Inhibition of Alt-Ej-mediated DNA repair in LIG4 knock out HEK293T cells
Inhibition of Alt-Ej-mediated DNA repair in LIG4 knock out HEK293T cells
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[PMID: 36126059] |
In Vitro
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[1].
RP-6685 inhibits Polθ in HEK293 LIG4-/- cellswith an IC50 of 0.94 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 nude mice (HCT116 BRCA2+/+ and BRCA2-/- xenograft tumor models)[1]
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Dosage:80 mg/kg
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Administration:p.o.; BID for 21 days
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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.
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Animal Model:CD1 mice (20-30 g)[1]
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Dosage:2.5 mg/kg
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Administration:i.v. or p.o.; single dosage
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Result:
CL (mL/min/kg) Vdss (L/kg) t1/2 (h) F (%) 36.8 1.1 0.4 66
Chemical Information
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CAS No. 2832047-80-8
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Appearance Solid
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Molecular Weight 497.37
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Formula C22H14F7N5O
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Color White to off-white
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SMILES
O=C(N(CC#CC1=NN=C(N)C=C1)C2=CC=C(F)C=C2)CC3=NC=C(C(F)(F)F)C=C3C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
HR eye & MMR eye: one-day assessment of DNA repair-defective tumors eligible for targeted therapy. [Abstract]2025 May 12;16(1):4239. PMID: 40355434 -
Cell Rep Med
2026 Mar 17;7(3):102687. PMID: 41850232 -
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bioRxiv
DNA polymerase theta-mediated DNA repair is a functional dependency and therapeutic vulnerability in DNMT3A deficient leukemia cells. [Abstract]2024 Sep 19:2024.09.15.613155. PMID: 39411165
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (201.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0106 mL | 10.0529 mL | 20.1058 mL | 50.2644 mL |
| 5 mM | 0.4021 mL | 2.0106 mL | 4.0212 mL | 10.0529 mL | |
| 10 mM | 0.2011 mL | 1.0053 mL | 2.0106 mL | 5.0264 mL | |
| 15 mM | 0.1340 mL | 0.6702 mL | 1.3404 mL | 3.3510 mL | |
| 20 mM | 0.1005 mL | 0.5026 mL | 1.0053 mL | 2.5132 mL | |
| 25 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0106 mL | |
| 30 mM | 0.0670 mL | 0.3351 mL | 0.6702 mL | 1.6755 mL | |
| 40 mM | 0.0503 mL | 0.2513 mL | 0.5026 mL | 1.2566 mL | |
| 50 mM | 0.0402 mL | 0.2011 mL | 0.4021 mL | 1.0053 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3351 mL | 0.8377 mL | |
| 80 mM | 0.0251 mL | 0.1257 mL | 0.2513 mL | 0.6283 mL | |
| 100 mM | 0.0201 mL | 0.1005 mL | 0.2011 mL | 0.5026 mL |
RP-6685 Related Classifications
HY-151462 Related Classifications
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