Home Cell Cycle CDK inhibitor - GSK-3 inhibitor - TAK1 inhibitor - JAK inhibitor - MEK inhibitor RGB-286638 free base

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RGB-286638 free base CDK inhibitor

Cat.No.E2821

RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
RGB-286638 free base CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 545.63

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: E282101 DMSO]100 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 98.26%
98.26

Chemical Information, Storage & Stability

Molecular Weight 545.63 Formula

C29H35N7O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 784210-88-4 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (183.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
cyclin T1-CDK9 [1]
(in kinase assay)
1 nM
cyclin B1-CDK1 [1]
(in kinase assay)
2 nM
cyclin E-CDK2 [1]
(in kinase assay)
3 nM
GSK-3β [1]
(in MTT assay)
3 nM
cyclin D1-CDK4 [1]
(in kinase assay)
4 nM
cyclin E-CDK3 [1]
(in kinase assay)
5 nM
p35-CDK5 [1]
(in kinase assay)
5 nM
TAK1 [1]
(in MTT assay)
5 nM
Jak2 [1]
(in MTT assay)
50 nM
MEK1 [1]
(in MTT assay)
54 nM
References

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