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RGB-286638 free base

Name: RGB-286638 free base
Brand: TargetMol
SKU: T2378
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2378Cas No. 784210-88-4

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

RGB-286638 free base

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Purity: 99.91%

Catalog No. T2378Cas No. 784210-88-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$39	In Stock	In Stock
2 mg	$55	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$278	In Stock	-
50 mg	$419	In Stock	-
100 mg	$587	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.91%

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

RGB-286638 free base AI Summary

RGB-286638 free base exhibits potent bioactivity by inhibiting various cyclin-dependent kinases (CDKs) including CDK7/cyclin H, CDK6/cyclin D3, CDK5/p35, CDK3/cyclin E, CDK2/cyclin E, recombinant CDK4/cyclin D1, CDK9/cyclin T1, and CDK1/cyclin B with IC50 values ranging from 1.0 nM to 4.0 nM. It also demonstrates notable antiviral activity, inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells by up to 70.16% and showing inhibition of the SARS-CoV-2 3CL-Pro protease. In addition, RGB-286638 free base displays inhibitory activity against the human HDAC6 enzyme. However, it also exhibits cytotoxicity against human HepG2 cells with an IC50 value of 200.0 nM. These multi-target bioactivities suggest that RGB-286638 free base has potential applications in oncology and antiviral therapies..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
Targets&IC50	JAK2:50 nM, CDK6-CyclinD3:55 nM, Cyclin T1-CDK9:1 nM, CDK5-p35:5 nM, c-Src:25 nM, JNK1a1:17 nM, Cyclin E-CDK3:5 nM, TAK1:5 nM, Cyclin D1-CDK4:4 nM, CDK7-CyclinH:44 nM, Cyclin E-CDK2:3 nM, MEK1:54 nM, Cyclin B1-CDK1:2 nM, AMPK:41 nM, JNK1a2:40 nM, GSK-3β:3 nM

Chemical Properties

Molecular Weight	545.63
Formula	C₂₉H₃₅N₇O₄
Cas No.	784210-88-4
Smiles	COCCN1CCN(Cc2ccc(cc2)-c2n[nH]c3-c4cccc(NC(=O)NN5CCOCC5)c4C(=O)c23)CC1
Relative Density.	1.39 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

0.1M HCl: 1 mg/mL (1.83 mM), Sonication is recommended.

DMSO: Slightly soluble

In Vivo Formulation

15% Solutol HS-15 in Saline: 10 mg/mL (18.33 mM), Suspension.

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

0.1M HCl

	1mg	5mg	10mg	50mg
1 mM	1.8327 mL	9.1637 mL	18.3274 mL	91.6372 mL

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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