K03861 (AUZ454)

Catalog No.S8100 Batch:S810002

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Technical Data

Formula

C24H26F3N7O2
Molecular Weight 501.50 CAS No. 853299-07-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (199.4 mM)
Ethanol 15 mg/mL (29.91 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description K03861 (AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
Targets
CDK2(C118L/A144C) [1]
(Cell-free assay)		 CDK2(A144C) [1]
(Cell-free assay)		 CDK2(C118L) [1]
(Cell-free assay)		 CDK2(WT) [1]
(Cell-free assay)
9.7 nM(Kd) 15.4 nM(Kd) 18.6 nM(Kd) 50 nM(Kd)
In vitro K03861 inhibits CDK2 activity by competing with binding of activating cyclins. [1]

Protocol (from reference)

Selleck's K03861 (AUZ454) has been cited by 15 publications

Functional Differentiation of Cyclins and Cyclin-Dependent Kinases in Giardia lamblia [ Microbiol Spectr, 2023, 11(2):e0491922] PubMed: 36877015
Functional Differentiation of Cyclins and Cyclin-Dependent Kinases in Giardia lamblia [ Microbiol Spectr, 2023, 11(2):e0491922] PubMed: 36877015
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151] PubMed: 35355016
p53 directs leader cell behavior, migration, and clearance during epithelial repair [ Science, 2022, 375(6581):eabl8876] PubMed: 35143293
Icaritin inhibits CDK2 expression and activity to interfere with tumor progression [ iScience, 2022, 25(9):104991] PubMed: 36093042
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] PubMed: 36248745
Transient inhibition of CDK2 activity prevents oocyte meiosis I completion and egg activation in mouse [ J Cell Physiol, 2022, 10.1002/jcp.30885] PubMed: 36161883
Postnatal expression and possible function of RANK and RANKL in the murine inner ear [ Bone, 2021, 145:115837] PubMed: 33385614
Tumors driven by RAS signaling harbor a natural vulnerability to oncolytic virus M1 [ Mol Oncol, 2020, 14(12):3153-3168] PubMed: 33037696
Tumors driven by RAS signaling harbor a natural vulnerability to oncolytic virus M1 [ Mol Oncol, 2020, 14(12):3153-3168] PubMed: 33037696

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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