Cat. No.: HY-126248

Tankyrase-IN-2

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Based on 1 Customer Validation

Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC₅₀s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.

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

Purity: 99.06%
CAS No.: 1588870-36-3
Formula: C₁₇H₁₄F₂N₂O₂
Molecular Weight:316.30

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tankyrase-IN-2 Chemical Structure

CAS No.: 1588870-36-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)^[1]

All PARP Isoforms :

All Wnt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf21	IC₅₀	782 nM Compound: 5k	Inhibition of recombinant human full-length Myc/His-tagged Parp-1 expressed in baculovirus infected Sf21 insect cells assessed as reduction in auto-PARsylation using activated DNA as substrate incubated for 150 mins in presence of NAD and bio-NAD as co-su Inhibition of recombinant human full-length Myc/His-tagged Parp-1 expressed in baculovirus infected Sf21 insect cells assessed as reduction in auto-PARsylation using activated DNA as substrate incubated for 150 mins in presence of NAD and bio-NAD as co-su	[PMID: 31381853]
Sf9	IC₅₀	>10 μM Compound: 5k	Inhibition of human N-terminal FLAG-tagged/C-terminal Strep-tagged PARP10 (805 to 1025 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method Inhibition of human N-terminal FLAG-tagged/C-terminal Strep-tagged PARP10 (805 to 1025 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	>10 μM Compound: 5k	Inhibition of human N-terminal GST-tagged PARP11 (8 to 338 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method Inhibition of human N-terminal GST-tagged PARP11 (8 to 338 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	>10 μM Compound: 5k	Inhibition of human N-terminal His/GST-tagged PARP12 (500 to 701 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method Inhibition of human N-terminal His/GST-tagged PARP12 (500 to 701 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated substrate by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	>10 μM Compound: 5k	Inhibition of N-terminal FLAG-tagged recombinant human PARP7 (400 to 657 residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal FLAG-tagged recombinant human PARP7 (400 to 657 residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	>10 μM Compound: 5k	Inhibition of N-terminal GST-tagged recombinant human full length PARP6 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal GST-tagged recombinant human full length PARP6 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	0.007 μM Compound: 5k	Inhibition of GST-tagged recombinant human TNKS2 (667 to 1166 end residues) expressed in baculovirus infected sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of GST-tagged recombinant human TNKS2 (667 to 1166 end residues) expressed in baculovirus infected sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	0.01 μM Compound: 5k	Inhibition of N-terminal GST-tagged recombinant human TNKS1 (1001 to 1327 end residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal GST-tagged recombinant human TNKS1 (1001 to 1327 end residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	0.71 μM Compound: 5k	Inhibition of N-terminal GST-tagged recombinant full length human PARP1 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal GST-tagged recombinant full length human PARP1 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	1 μM Compound: 5k	Inhibition of N-terminal GST-tagged recombinant human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal GST-tagged recombinant human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	1.9 μM Compound: 5k	Inhibition of N-terminal GST-tagged recombinant full length human PARP3 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method Inhibition of N-terminal GST-tagged recombinant full length human PARP3 expressed in Baculovirus infected Sf9 cells using biotinylated substrate after 1 hr by chemiluminescence method	[PMID: 31381853]
Sf9	IC₅₀	7 nM Compound: 5k	Inhibition of GST tagged-TEV cleavage site-fused human recombinant TNKS1 (1023 to 1327 residues) expressed in baculovirus infected sf9 cells assessed as reduction in auto-PARsylation incubated for 1 hr in presence of bio-NAD as co-substrate by ELISA Inhibition of GST tagged-TEV cleavage site-fused human recombinant TNKS1 (1023 to 1327 residues) expressed in baculovirus infected sf9 cells assessed as reduction in auto-PARsylation incubated for 1 hr in presence of bio-NAD as co-substrate by ELISA	[PMID: 31381853]
Sf9	IC₅₀	9.2 nM Compound: 5k	Inhibition of GST tagged-TEV cleavage site-fused human recombinant TNKS2 (873 to 1166 residues) expressed in baculovirus infected sf9 cells assessed as reduction in auto-PARsylation incubated for 60 mins in presence of bio-NAD as co-substrate by ELISA Inhibition of GST tagged-TEV cleavage site-fused human recombinant TNKS2 (873 to 1166 residues) expressed in baculovirus infected sf9 cells assessed as reduction in auto-PARsylation incubated for 60 mins in presence of bio-NAD as co-substrate by ELISA	[PMID: 31381853]

In Vitro

Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC₅₀ of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC₅₀=319 nM)^[1].

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

Chemical Information

CAS No. 1588870-36-3
Appearance Solid
Molecular Weight 316.30
Formula C₁₇H₁₄F₂N₂O₂
Color White to off-white
SMILES

O=C1NC(C2=CC=C(C(C)(O)C)C=C2)=NC3=C1C=C(F)C=C3F
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (263.45 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

3.1616 mL

15.8078 mL

31.6156 mL

5 mM

0.6323 mL

3.1616 mL

6.3231 mL

10 mM

0.3162 mL

1.5808 mL

3.1616 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.58 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective TankyraseInhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019 Aug 5. [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

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1616 mL	15.8078 mL	31.6156 mL	79.0389 mL
	5 mM	0.6323 mL	3.1616 mL	6.3231 mL	15.8078 mL
	10 mM	0.3162 mL	1.5808 mL	3.1616 mL	7.9039 mL
	15 mM	0.2108 mL	1.0539 mL	2.1077 mL	5.2693 mL
	20 mM	0.1581 mL	0.7904 mL	1.5808 mL	3.9519 mL
	25 mM	0.1265 mL	0.6323 mL	1.2646 mL	3.1616 mL
	30 mM	0.1054 mL	0.5269 mL	1.0539 mL	2.6346 mL
	40 mM	0.0790 mL	0.3952 mL	0.7904 mL	1.9760 mL
	50 mM	0.0632 mL	0.3162 mL	0.6323 mL	1.5808 mL
	60 mM	0.0527 mL	0.2635 mL	0.5269 mL	1.3173 mL
	80 mM	0.0395 mL	0.1976 mL	0.3952 mL	0.9880 mL
	100 mM	0.0316 mL	0.1581 mL	0.3162 mL	0.7904 mL

Keywords

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Tankyrase-IN-2

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound 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

All PARP Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tankyrase-IN-2

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound 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

All PARP Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tankyrase-IN-2 Related Classifications

HY-126248 Related Classifications