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MC180295 CDK inhibitor

Cat.No.S8809

MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for this compound over other CDKs.
MC180295 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 358.41

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 358.41 Formula

C17H18N4O3S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2237942-08-2 -- Storage of Stock Solutions

Synonyms (rel)-MC180295 Smiles C1CC2CC1CC2NC3=NC(=C(S3)C(=O)C4=CC=CC=C4[N+](=O)[O-])N

Solubility

In vitro
Batch:

DMSO : 72 mg/mL ( (200.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 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
CDK9-Cyclin T1 [1]
(Cell-free assay)
5 nM
CDK4-Cyclin D [1]
(Cell-free assay)
112 nM
CDK1-Cyclin B [1]
(Cell-free assay)
138 nM
CDK5-P35 [1]
(Cell-free assay)
159 nM
CDK5-P25 [1]
(Cell-free assay)
186 nM
CDK2-Cyclin A [1]
(Cell-free assay )
233 nM
CDK2-Cyclin E [1]
(Cell-free assay)
367 nM
CDK3-Cyclin E [1]
(Cell-free assay)
399 nM
In vitro

This compound has broad anti-cancer activity in vitro[1].
In vivo

MC180295 shows promising anti-tumoral and immunosensitization activity[1].
References

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