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GP-82996 (Alias: CINK4, Cdk4/6 Inhibitor IV)

Name: GP-82996
Brand: TargetMol
SKU: T21720
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T21720 Copy Product Info

Purity: 99.94%

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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].

GP-82996

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Catalog No. T21720

Alias CINK4, Cdk4/6 Inhibitor IV

Cas No. 359886-84-3

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Pack Size	Price	USA Stock	Global Stock
1 mg	$43	In Stock	In Stock
5 mg	$171	In Stock	In Stock
10 mg	$301	In Stock	In Stock
25 mg	$612	In Stock	In Stock
50 mg	$867	In Stock	In Stock
100 mg	$1,160	In Stock	In Stock

In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.94%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

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].
Targets&IC50	V-abl:>10 μM, Cdk4-CyclinD1:1.5 μM, CDK5-p35:25 μM, CDK2-CyclinA:>50 μM, CDK6-CyclinD1:5.6 μM, CDK2-CyclinE:>50 μM, IGF-1R:>10 μM, Insulin Receptor:>10 μM, CDK6-CyclinD2:>50 μM, c-Met:>10 μM, CDK1-cyclinB:>100 μM, CDK4-CyclinD2:>50 μM
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) significantly reduced final tumor volume compared to the vehicle control in mouse xenograft models [1]. In female BALB/c nu/nu mice (19-21 g) with HCT116 tumors (100 mm^3), the compound was administered intraperitoneally at 30 mg/kg every 12 hours for 29 days, leading to smaller tumor volumes than the control group [1].
Synonyms	CINK4, Cdk4/6 Inhibitor IV

Chemical Properties

Molecular Weight	456.58
Formula	C₂₇H₃₂N₆O
Cas No.	359886-84-3
Smiles	C(N1C=2C(=CC(NC=3N=C(N[C@@H]4CC[C@@H](O)CC4)C=C(NCC)N3)=CC2)C=C1)C5=CC=CC=C5
Relative Density.	1.28 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (109.51 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.38 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1902 mL	10.9510 mL	21.9020 mL	109.5098 mL
5 mM	0.4380 mL	2.1902 mL	4.3804 mL	21.9020 mL
10 mM	0.2190 mL	1.0951 mL	2.1902 mL	10.9510 mL
20 mM	0.1095 mL	0.5475 mL	1.0951 mL	5.4755 mL
50 mM	0.0438 mL	0.2190 mL	0.4380 mL	2.1902 mL
100 mM	0.0219 mL	0.1095 mL	0.2190 mL	1.0951 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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