Home Cell Cycle CDK4/6 inhibitor Auceliciclib (AU3-14,Ulecaciclib )

research use only

Auceliciclib (AU3-14,Ulecaciclib ) CDK4/6 inhibitor

Ulecaciclib is an orally active cyclin-dependent kinase (CDK) inhibitor with Ki values of 0.62 μM for CDK2/Cyclin A, 0.2 nM for CDK4/Cyclin D1, 3 nM for CDK6/Cyclin D3, and 0.63 μM for CDK7/Cyclin H. This compound demonstrates blood-brain barrier penetration and favorable pharmacokinetic properties.

Auceliciclib (AU3-14,Ulecaciclib ) CDK4/6 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 496.65

Purity & Quality Control

Related Products

Mechanism of Action

In Vivo
In vivo Ulecaciclib (compound 2) (2 mg/kg for i.v.; 10 mg/kg for p.o.) demonstrates a significantly propensity to cross the blood brain barrier in mice, with the brain/plasma ratios are >1.2 (i.v.) or >0.7 (p.o.), respectively. Ulecaciclib (200 mg/kg; p.o.; daily; 21 d) displays in vivo anti-tumour efficacy in mice. Ulecaciclib (25 mg/kg; p.o.; daily; 10 d) demonstrates significant anti-tumour efficacy at lower doses in combination with TMZ (5 mg/kg; p.o.; 5 d/week; 2 weeks) in mice. Ulecaciclib (compound A) (50 mg/kg; p.o.) shows an oral bioavailability of about 21.8%, and good pharmacokinetic profile with Tmax of 6.67 h and an half- of 8.34 h, while Cmax =643 ng/mL, AUC(0-24) =9543 ng•h/mL in male cynomolgus monkeys. Pharmacokinetic of Ulecaciclib in cynomolgus monkeys

References
  • https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl127.pdf?sfvrsn=8544ca1e_3&download=true
  • https://www.freepatentsonline.com/WO2021222967A1.html
  • https://www.freepatentsonline.com/WO2022099357A1.html

Chemical Information

Molecular Weight 496.65 Formula

C25H33FN8S
CAS No. 2075750-05-7 SDF Download SDF
Smiles FC1=C(C2=C(C)N=C(NC3CCCC3)S2)N=C(NC4=NC=C(CN5CCN(CC5)CC)C=C4)N=C1

Storage and Stability

Storage (From the date of receipt)

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.