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    Epigenetics
  2. PARP
  3. RK-287107

RK-287107 

Cat. No.: HY-123892
Handling Instructions

RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.

For research use only. We do not sell to patients.

RK-287107 Chemical Structure

RK-287107 Chemical Structure

CAS No. : 2171386-10-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth[1].

IC50 & Target[1]

tankyrase-1

14.3 nM (IC50)

tankyrase-2

10.6 nM (IC50)

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[1].
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1].
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1].

Cell Proliferation Assay[1]

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[1]

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
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[1].

Animal Model: 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1]
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.
Molecular Weight

416.46

Formula

C₂₂H₂₆F₂N₄O₂

CAS No.

2171386-10-8

SMILES

O=C1NC(N2CCC3(CC2)CN(CCO)C4=C3C(F)=CC(F)=C4)=NC5=C1CCCC5

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (300.15 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4012 mL 12.0060 mL 24.0119 mL
5 mM 0.4802 mL 2.4012 mL 4.8024 mL
10 mM 0.2401 mL 1.2006 mL 2.4012 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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RK-287107
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