Cat. No.: HY-123892

RK-287107

1 Cited Publications

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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.

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Pureté: 99.80%
CAS No.: 2171386-10-8
Formule: C₂₂H₂₆F₂N₄O₂
Masse moléculaire:416.46

Stockage:

4°C, protect from light

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

RK-287107 Chemical Structure

CAS No.: 2171386-10-8

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

tankyrase-1

14.3 nM (IC₅₀)

tankyrase-2

10.6 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PARP :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 320DM	GI₅₀	0.45 μM Compound: 1; RK-287107	Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 32202790]
COLO 320DM	GI₅₀	0.45 μM Compound: 40c; RK-287107	Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 30883102]
COLO 320DM	GI₅₀	1.6 μM Compound: 40c; RK-287107	Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay	[PMID: 30883102]
COLO 320DM	GI₅₀	1.63 μM Compound: 1; RK-287107	Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay	[PMID: 32202790]
HEK293	IC₅₀	12.1 nM Compound: 1; RK-287107	Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay	[PMID: 32202790]
HEK293	IC₅₀	12.1 nM Compound: 40c; RK-287107	Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay	[PMID: 30883102]
RKO	GI₅₀	>10 μM Compound: 1; RK-287107	Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 32202790]
RKO	GI₅₀	>10 μM Compound: 40c; RK-287107	Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 30883102]
Sf9	IC₅₀	2717 nM Compound: 1; RK-287107	Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS	[PMID: 32202790]
Sf9	IC₅₀	2717 nM Compound: 40c; RK-287107	Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS	[PMID: 30883102]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6-week-old female NOD.CB17-Prkdc^scid/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.

Chemical Information

CAS No. 2171386-10-8
Appearance Solid
Masse moléculaire 416.46
Formule C₂₂H₂₆F₂N₄O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Publications (1)

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Journal Impact Factor

Am J Cancer Res

TNKS inhibitors potentiate proliferative inhibition of BET inhibitors via reducing β-Catenin in colorectal cancer cells. [Abstract]

2022 Mar 15;12(3):1069-1087. PMID: 35411247

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (240.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mizutani A, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci. 2018 Dec;109(12):4003-4014. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4012 mL	12.0060 mL	24.0119 mL	60.0298 mL
	5 mM	0.4802 mL	2.4012 mL	4.8024 mL	12.0060 mL
	10 mM	0.2401 mL	1.2006 mL	2.4012 mL	6.0030 mL
	15 mM	0.1601 mL	0.8004 mL	1.6008 mL	4.0020 mL
	20 mM	0.1201 mL	0.6003 mL	1.2006 mL	3.0015 mL
	25 mM	0.0960 mL	0.4802 mL	0.9605 mL	2.4012 mL
	30 mM	0.0800 mL	0.4002 mL	0.8004 mL	2.0010 mL
	40 mM	0.0600 mL	0.3001 mL	0.6003 mL	1.5007 mL
	50 mM	0.0480 mL	0.2401 mL	0.4802 mL	1.2006 mL
	60 mM	0.0400 mL	0.2001 mL	0.4002 mL	1.0005 mL
	80 mM	0.0300 mL	0.1501 mL	0.3001 mL	0.7504 mL
	100 mM	0.0240 mL	0.1201 mL	0.2401 mL	0.6003 mL

Keywords

RK-287107

1 Cited Publications

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RK-287107

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RK-287107

Voir tous les produits spécifiques à Isoform PARP

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RK-287107

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Anti-Colorectal Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RK-287107

Voir tous les produits spécifiques à Isoform PARP

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RK-287107 Related Classifications

HY-123892 Related Classifications