K03861

CDK2 inhibitor CAS# 853299-07-7

K03861

Catalog No. BCC6537----Order now to get a substantial discount!

Product Name & Size Price Stock
K03861: 5mg $150 In Stock
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Quality Control of K03861

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Chemical structure

K03861

3D structure

Chemical Properties of K03861

Cas No. 853299-07-7 SDF Download SDF
PubChem ID 11260561 Appearance Powder
Formula C24H26F3N7O2 M.Wt 501.5
Type of Compound N/A Storage Desiccate at -20°C
Solubility >50.2mg/mL in DMSO
Chemical Name 1-[4-(2-aminopyrimidin-4-yl)oxyphenyl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]urea
SMILES CN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)NC3=CC=C(C=C3)OC4=NC(=NC=C4)N)C(F)(F)F
Standard InChIKey PWDLXPJQFNVTNL-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H26F3N7O2/c1-33-10-12-34(13-11-33)15-16-2-3-18(14-20(16)24(25,26)27)31-23(35)30-17-4-6-19(7-5-17)36-21-8-9-29-22(28)32-21/h2-9,14H,10-13,15H2,1H3,(H2,28,29,32)(H2,30,31,35)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of K03861

DescriptionK03861 is a type II CDK2 inhibitor with Kd of 8.2 nM. K03861 inhibits CDK2 activity by competing with binding of activating cyclins.

References:
[1]. Alexander LT et al. Type II Inhibitors Targeting CDK2. ACS Chem Biol. 2015 Sep 18;10(9):2116-25.

K03861 Dilution Calculator

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K03861 Molarity Calculator

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Preparing Stock Solutions of K03861

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.994 mL 9.9701 mL 19.9402 mL 39.8804 mL 49.8504 mL
5 mM 0.3988 mL 1.994 mL 3.988 mL 7.9761 mL 9.9701 mL
10 mM 0.1994 mL 0.997 mL 1.994 mL 3.988 mL 4.985 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.7976 mL 0.997 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.3988 mL 0.4985 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on K03861

K03861 is a type II inhibitor of CDK2. The cyclin-dependent kinase holoenzymes contain a catalytic subunit, the Cdk, a family of regulatory subunits, and the cyclins. Cdks are the catalytic subunits of the mammalian heterodimeric serine/threonine kinases progression, Cyclin-dependent kinases (CDKs) play important roles in the cell cycle regulation, transcription, and neuronal function. CDKs are frequently deregulated in some human tumours. The inhibitors targeted CDK are thought to prevent cell proliferation regulating cyclin-CDK complexes. The central role of CDKs in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the cell proliferation [1].

K03861 is an aminopyrimidine-phenyl urea inhibitor of CDK2. The type II inhibitor CDK2 cocrystal structure of CDK2 with the inhibitor K03861 revealed a canonical type II binding mode. The type II inhibitors could compete with the binding of cyclins. The residues important for the type II inhibitors may be distant to the ATP binding pockets. The crystal structure of this complex may provide a foundation for the cyclin-competitive CDK2 inhibitors [2].

References:
Malumbres M, Barbacid M.  Mammalian cyclin-dependent kinases[J]. Trends in biochemical sciences, 2005, 30(11): 630-641.
Alexander L T, Mo?bitz H, Drueckes P, et al.  Type II inhibitors targeting CDK2[J]. ACS chemical biology, 2015, 10(9): 2116-2125.

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References on K03861

Type II Inhibitors Targeting CDK2.[Pubmed:26158339]

ACS Chem Biol. 2015 Sep 18;10(9):2116-25.

Kinases can switch between active and inactive conformations of the ATP/Mg(2+) binding motif DFG, which has been explored for the development of type I or type II inhibitors. However, factors modulating DFG conformations remain poorly understood. We chose CDK2 as a model system to study the DFG in-out transition on a target that was thought to have an inaccessible DFG-out conformation. We used site-directed mutagenesis of key residues identified in structural comparisons in conjunction with biochemical and biophysical characterization of the generated mutants. As a result, we identified key residues that facilitate the DFG-out movement, facilitating binding of type II inhibitors. However, surprisingly, we also found that wild type CDK2 is able to bind type II inhibitors. Using protein crystallography structural analysis of the CDK2 complex with an aminopyrimidine-phenyl urea inhibitor (K03861) revealed a canonical type II binding mode and the first available type II inhibitor CDK2 cocrystal structure. We found that the identified type II inhibitors compete with binding of activating cyclins. In addition, analysis of the binding kinetics of the identified inhibitors revealed slow off-rates. The study highlights the importance of residues that may be distant to the ATP binding pocket in modulating the energetics of the DFG-out transition and hence inhibitor binding. The presented data also provide the foundation for a new class of slow off-rate cyclin-competitive CDK2 inhibitors targeting the inactive DFG-out state of this important kinase target.

Description

AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.

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