2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. RP-6685

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.

RP-6685 Chemical Structure

RP-6685 Chemical Structure

CAS No. : 2832047-80-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 218 In-stock
Solution
10 mM * 1 mL in DMSO USD 218 In-stock
Solid
1 mg USD 100 In-stock
5 mg USD 199 In-stock
10 mg USD 296 In-stock
25 mg USD 492 In-stock
50 mg USD 685 In-stock
100 mg USD 960 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

RP-6685 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE RP-6685

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

IC50: 5.8 nM (Polθ)[1]
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.

RP-6685 Related Antibodies
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) Vdss (L/kg) t1/2 (h) F (%)
36.8 1.1 0.4 66
Molecular Weight

497.37

Formula

C22H14F7N5O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0106 mL 10.0529 mL 20.1058 mL
5 mM 0.4021 mL 2.0106 mL 4.0212 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.96%

COA (247 KB) HNMR (283 KB) LCMS (264 KB)

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
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RP-6685 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RP-66852832047-80-8RP6685RP 6685DNA/RNA SynthesisantitumorHCT116BRCA2xenograftCD1 nude miceInhibitorinhibitorinhibit

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