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LDC000067 CDK inhibitor

Cat.No.S7461

LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
LDC000067 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 370.43

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 370.43 Formula

C18H18N4O3S

Storage (From the date of receipt)
CAS No. 1073485-20-7 Download SDF Storage of Stock Solutions

Synonyms LDC067 Smiles COC1=CC=CC=C1C2=CC(=NC=N2)NC3=CC=CC(=C3)CS(=O)(=O)N

Solubility

In vitro
Batch:

DMSO : 74 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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

Features
CDK9-selective inhibitor.
Targets/IC50/Ki
CDK9 [1]
(Cell-free assay)
44 nM
CDK2 [1]
(Cell-free assay)
2.441 μM
In vitro
LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo RNA synthesis of cellular genes.[1]
References

Applications

Methods Biomarkers Images PMID
Western blot CDK9 / RNAPII / p-RNAPII / MCL-1 / BIRC5 S7461-WB1 30579871

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