Home DNA Damage/DNA Repair PARP inhibitor RK-287107 For research use only.

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.

RK-287107 Chemical Structure

RK-287107 Chemical Structure

CAS No. 2171386-10-8

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RK-287107 Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 416.46 Formula

C22H26F2N4O2
CAS No. 2171386-10-8 SDF --
Smiles C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (199.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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In vivo
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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.

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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.

Handling Instructions

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