RK-287107

Catalog No.S8876

For research use only.

RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM.

RK-287107 Chemical Structure

CAS No. 2171386-10-8

Purity & Quality Control

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Biological Activity

Description RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM.
Targets
Tankyrase-2 [1]
(Cell-free assay)
Tankyrase-1 [1]
(Cell-free assay)
10.6 nM 14.3 nM
In vitro

RK-287107 is a novel tankyrase-specific inhibitor that inhibits tankyrase-1 and -2. RK-287107 causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations. Consistently, RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells.[1]

In vivo

Intraperitoneal or oral administration of RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice. RK-287107 suppresses the Wnt/β-catenin pathway and tumor growth of the xenografted COLO-320DM cells in vivo.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: COLO-320DM, HCC2998, HCT-116, DLD-1, SW403, RKO
  • Concentrations: 0.01-10 μM
  • Incubation Time: 120 h
  • Method:

    Cells are treated with RK-287107 in triplicate for 120 h. Relative cell number is quantitated by MTT assays. Experiments are repeated at least twice and the average values are plotted.

Animal Research:

[1]

  • Animal Models: 6-week-old female NOD.CB17-Prkdcscid/J mice s.c. injected with COLO-320DM cells
  • Dosages: 100 mg/kg, 150 mg/kg, 300 mg/kg
  • Administration: IP, Oral gavage

Solubility (25°C)

In vitro

DMSO 83 mg/mL
(199.29 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL

Chemical Information

Molecular Weight 416.46
Formula

C22H26F2N4O2

CAS No. 2171386-10-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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