RK-287107 - 98%, high purity , CAS No.2171386-10-8, Inhibitor of tankyrase;Inhibitor of tankyrase 2

Item Number

R414236

• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Protected from light,Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of tankyrase;Inhibitor of tankyrase 2

Product Description

Information

RK-287107 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 (Cell-free assay); Tankyrase-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.

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.

Cell Research(from reference)

Cell lines：COLO-320DM, HCC2998, HCT-116, DLD-1, SW403, RKO 

Concentrations：0.01-10 μM 

Incubation Time：120 h