2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. RK-582

RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model.

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RK-582

RK-582 Chemical Structure

CAS No. : 2171388-28-4

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Based on 1 publication(s) in Google Scholar

RK-582 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model[1].

IC50 & Target

IC50: 36.1 nM (TNKS1/PARP5A), 18.168 nM (PARP1)[1]
Cellular Effect
Cell Line Type Value Description References
COLO 320 GI50
230 nM
Compound: 35; RK-582
Antiproliferative activity against human COLO 320 assessed as growth inhibition measured after 24 hrs
Antiproliferative activity against human COLO 320 assessed as growth inhibition measured after 24 hrs
[PMID: 33822624]
COLO 320DM GI50
0.035 μM
Compound: 41g; RK-582
Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay
Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay
[PMID: 32202790]
COLO 320DM GI50
0.23 μM
Compound: 41g; RK-582
Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
[PMID: 32202790]
HEK293 IC50
0.3 nM
Compound: 41g; RK-582
Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay
Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay
[PMID: 32202790]
RKO GI50
> 10 μM
Compound: 41g; RK-582
Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay
Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay
[PMID: 32202790]
Sf9 IC50
1240 nM
Compound: 41g; RK-582
Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS
Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS
[PMID: 32202790]
Clinical Trial
Molecular Weight

510.60

Formula

C27H35FN6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C)C2(CCN(C(NC3=C4CCCN3C)=NC4=O)CC2)C(C1=CC(N(C[C@@H]5C)C[C@H](O5)C)=C6)=C6F
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 : 25 mg/mL (48.96 mM; ultrasonic and warming and heat to 60°C; 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 1.9585 mL 9.7924 mL 19.5848 mL
5 mM 0.3917 mL 1.9585 mL 3.9170 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.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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
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 1.9585 mL 9.7924 mL 19.5848 mL 48.9620 mL
5 mM 0.3917 mL 1.9585 mL 3.9170 mL 9.7924 mL
10 mM 0.1958 mL 0.9792 mL 1.9585 mL 4.8962 mL
15 mM 0.1306 mL 0.6528 mL 1.3057 mL 3.2641 mL
20 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4481 mL
25 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9585 mL
30 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6321 mL
40 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
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RK-582 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:

RK-5822171388-28-4RK582RK 582PARPpoly ADP ribose polymeraseoral effectivexenograft modelCOLO-320DMInhibitorinhibitorinhibit

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