RK-287107

For research use only.

Catalog No.S8876

RK-287107 Chemical Structure

CAS No. 2171386-10-8

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.

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 416.46
Formula

C22H26F2N4O2

CAS No. 2171386-10-8
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID