Home Tools

GP-82996

Catalog No. T21720 CAS 359886-84-3

Synonyms: Cdk4/6 Inhibitor IV, CINK4

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GP-82996, CAS 359886-84-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 178.00
25 mg	In stock	$ 369.00
50 mg	In stock	$ 588.00
100 mg	In stock	$ 926.00

Bulk Inquiry

Select Batch

Purity: 99.57%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].
In vitro	GP-82996, at concentrations of 5 and 10 μM applied for 24 hours, causes a G1 phase arrest and an increase in the G0-G1/S ratio in U2OS (p16 negative) and MRC-5 (p16 positive) cells, while reducing the hyperphosphorylation of pRb without affecting CDK4 levels in these cell lines. In U2OS cells, a 48-hour exposure to 10μM of GP-82996 results in apoptosis in 83% of the population. Additionally, GP-82996 inhibits the proliferation of A549, H358, SKLU-1, H23, and PC14 cells, with IC50 values around 4-7 μM after 72 hours of treatment. The compound also induces G1 arrest in A549 and H23 cells at concentrations of 3, 5, and 10 μM over 48 hours and enhances the sensitivity of KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23) to Paclitaxel with varied concentrations (1, 3, 5, 10 μM) over 72 hours. A combination of GP-82996 (10 μM) and Paclitaxel (3 nM) over 72 hours notably increases apoptosis in A549 and H23 cells.
In vivo	GP-82996 (30 mg/kg, i.p. for 29 days) demonstrated a reduction in final tumor volume compared to the vehicle control in mouse xenograft models [1]. Utilizing female BALB/c nu/nu mice, weighing 19-21 g, with HCT116 tumors measuring 100 mm^3, the compound was administered intraperitoneally (i.p.) at a dosage of 30 mg/kg every 12 hours over a period of 29 days, resulting in noticeably smaller final tumor volumes in comparison to those observed in the vehicle control group [1].

Synonyms	Cdk4/6 Inhibitor IV, CINK4
Molecular Weight	456.58
Formula	C27H32N6O
CAS No.	359886-84-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27mg/mL (59.1mM)

References and Literature

1. Soni R, et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J Natl Cancer Inst. 2001 Mar 21;93(6):436-46. 2. Zhang XH, et al. A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS. Cancer Biol Ther. 2013;14(7):597-605.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library Kinase Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

CDK8-IN-12 CDK1-IN-2 SU9516 (S)-Enitociclib SHR5428 Abemaciclib methanesulfonate CDK9-IN-10 InhA-IN-2

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GP-82996 359886-84-3 Cell Cycle/Checkpoint CDK GP82996 CINK-4 Cdk4/6 Inhibitor IV CINK4 GP 82996 CINK 4 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.