RK-287107

Catalog No.S8876 Batch:S887602

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Technical Data

Formula

C22H26F2N4O2
Molecular Weight 416.46 CAS No. 2171386-10-8
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.