RK-287107

SKU: orb1218434

Description

RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).

Key Properties

• CAS Number: 2171386-10-8
• MW: 416.46
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₆F₂N₄O₂
• SMILES: OCCN(C1)c2cc(F)cc(F)c2C1(CC1)CCN1C(N1)=NC(CCCC2)=C2C1=O
• Target: tankyrase 1|tankyrase 2
• Solubility: DMSO:120 mg/mL (288.14 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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 in a mouse xenograft model. Animal model: 6-week-old female NOD. CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM. Dosage: 100 and 300 mg/kg. Administration: Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks. Result: 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.
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• In Vitro:
  RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells. Cell Proliferation Assay Cell line: Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells. Concentration: 0.01, 0.1, 1, 10 μM Incubation time: 12 hours. Result: Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1. Western blot analysis. Cell line: COLO-320DM cells. Concentration: 0.03, 0.1, 0.33, 1, 3, and 10 μM Incubation time: 16 hours. Result: Downregulation of active β-catenin was observed
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

tankyrase 1|tankyrase 2