Cat. No.: HY-180896

8012–3246

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Based on 1 Customer Validation

8012-3246 is a selective PLK2 inhibitor with an IC₅₀ of 774.5 nM. 8012-3246 suppresses GSK3β phosphorylation. 8012-3246 exhibits potent anticancer activity against colorectal cancer.

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

Purity: 99.72%
CAS No.: 421586-94-9
Formula: C₁₈H₁₃N₅O₃
Molecular Weight:347.33

Storage:

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

8012–3246 Chemical Structure

CAS No.: 421586-94-9

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

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

Biological Activity

Description

8012-3246 is a selective PLK2 inhibitor with an IC₅₀ of 774.5 nM. 8012-3246 suppresses GSK3β phosphorylation. 8012-3246 exhibits potent anticancer activity against colorectal cancer^[1].

IC₅₀ & Target^[1]

GSK-3β

PLK2

774.5 nM (IC₅₀)

All Polo-like Kinase (PLK) Isoforms :

All GSK-3 Isoforms :

Chemical Information

CAS No. 421586-94-9
Appearance Solid
Molecular Weight 347.33
Formula C₁₈H₁₃N₅O₃
Color Off-white to light brown
SMILES

NC1=C(C#N)C(C(C(C2=CC=NC=C2)=NN3)=C3O1)C4=CC=C(O)C(O)=C4
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 : 100 mg/mL (287.91 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

2.8791 mL

14.3955 mL

28.7911 mL

5 mM

0.5758 mL

2.8791 mL

5.7582 mL

10 mM

0.2879 mL

1.4396 mL

2.8791 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)

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (280 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]. Wu YW, et al. Consensus Pharmacological Interactions for PLK2 Inhibitor Identification in Colorectal Cancer Treatment. J Chem Inf Model. 2026 Jan 12;66(1):577-590. [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	2.8791 mL	14.3955 mL	28.7911 mL	71.9777 mL
	5 mM	0.5758 mL	2.8791 mL	5.7582 mL	14.3955 mL
	10 mM	0.2879 mL	1.4396 mL	2.8791 mL	7.1978 mL
	15 mM	0.1919 mL	0.9597 mL	1.9194 mL	4.7985 mL
	20 mM	0.1440 mL	0.7198 mL	1.4396 mL	3.5989 mL
	25 mM	0.1152 mL	0.5758 mL	1.1516 mL	2.8791 mL
	30 mM	0.0960 mL	0.4799 mL	0.9597 mL	2.3993 mL
	40 mM	0.0720 mL	0.3599 mL	0.7198 mL	1.7994 mL
	50 mM	0.0576 mL	0.2879 mL	0.5758 mL	1.4396 mL
	60 mM	0.0480 mL	0.2399 mL	0.4799 mL	1.1996 mL
	80 mM	0.0360 mL	0.1799 mL	0.3599 mL	0.8997 mL
	100 mM	0.0288 mL	0.1440 mL	0.2879 mL	0.7198 mL

Keywords

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8012–3246

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

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Wnt/Hedgehog/Notch Compound Library

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Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

All Polo-like Kinase (PLK) Isoforms

All GSK-3 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

8012–3246 Related Classifications

HY-180896 Related Classifications