RK-287107

SKU: orb1307790

Description

RK-287107 is a potent and selective tankyrase inhibitor, demonstrating IC50 values of 14.3 nM and 10.6 nM against tankyrase-1 and tankyrase-2, respectively. This small molecule is a valuable research tool for studying Wnt/β-catenin signaling in cancer biology and has been utilized in both cellular and in vivo models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 2171386-10-8
• MW: 416.46
• Purity: 99.59% (May vary between batches)
• Formula: C₂₂H₂₆F₂N₄O₂
• SMILES: OCCN1CC2(CCN(CC2)c2nc3CCCCc3c(=O)[nH]2)c2c1cc(F)cc2F
• Target: PARP
• Solubility: DMSO:120 mg/mL (288.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.6 mM)

Bioactivity

• Target IC50:
  Tankyrase 2:10.6 nM|Tankyrase 1:14.3 nM
• In Vivo:
  In a mouse xenograft model, RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth .
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• In Vitro:
  RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells. 287107 (0.03-10 μM; 16 hours) induces the accumulation of tankyrase and Axin1/2. RK-87107 (0.01-10 μM; 12 hours) displays an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK- .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PARP, inhibit, Inhibitor, tankyrase 1, tankyrase 2, tankyrase-1, tankyrase-2, RK 287107, RK287107, RK-287107, poly ADP ribose polymerase

Compound Identifiers

PubChem CID

137701512