Cat. No.: HY-151462

RP-6685

3 Cited Publications

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Based on 3 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.

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Pureté: 99.88%
CAS No.: 2832047-80-8
Formule: C₂₂H₁₄F₇N₅O
Masse moléculaire:497.37

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RP-6685 Chemical Structure

CAS No.: 2832047-80-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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^[1]. 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.

IC₅₀ & Target

DNA Polymerase

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	>15 μM Compound: RP-6685	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	[PMID: 36126059]
HCT-116	IC₅₀	0.32 μM Compound: RP-6685	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	[PMID: 36126059]
HCT-116	IC₅₀	0.45 μM Compound: RP-6685	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	[PMID: 36126059]
HEK-293T	IC₅₀	2.147 x 10^-6 M Compound: RP-6685	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	[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.

In Vivo

RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice^[1].

MedChemExpress (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)^[1]
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)^[1]
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

Chemical Information

CAS No. 2832047-80-8
Appearance Solid
Masse moléculaire 497.37
Formule C₂₂H₁₄F₇N₅O
Color White to off-white
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

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

Polθ activity modulates sensitivity to standard therapies in DNMT3A-deficient leukemia. [Abstract]

2026 Mar 17;7(3):102687. PMID: 41850232
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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0106 mL

10.0529 mL

20.1058 mL

5 mM

0.4021 mL

2.0106 mL

4.0212 mL

10 mM

0.2011 mL

1.0053 mL

2.0106 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

RP-6685

3 Cited Publications

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RP-6685

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) RP-6685

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CL (mL/min/kg)	V_dss (L/kg)	t_1/2 (h)	F (%)
36.8	1.1	0.4	66

RP-6685

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) RP-6685

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RP-6685 Related Classifications

HY-151462 Related Classifications