2. Cell Cycle/DNA Damage
  3. CDK
  4. AUZ 454

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.

For research use only. We do not sell to patients.

AUZ 454 Chemical Structure

AUZ 454 Chemical Structure

CAS No. : 853299-07-7

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5 mg USD 90 In-stock
10 mg USD 144 In-stock
25 mg USD 300 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
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Based on 4 publication(s) in Google Scholar

AUZ 454 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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.

IC50 & Target[1]

CDK2(C118L/A144C)

9.7 nM (Kd)

CDK2(A144C)

15.4 nM (Kd)

CDK2(C118L)

18.6 nM (Kd)

CDK2(WT)

50 nM (Kd)

CDK2(C118L/A144C-Cyclin B)

134.1 nM (Kd)

In Vitro

AUZ 454 (K03861) (10-20 μM; 1, 2, 3, and 4 days) has a inhibitory effect on Caki-1 and ACHN cells with WTAP overexpression by CCK8 assays[2].
AUZ 454 (K03861) (10 μM; 24 hours) decreases the colony fold in Caki-1 and ACHN cells through a CDK2-dependent mechanism[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AUZ 454 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: Caki-1 and ACHN cells
Concentration: 10 μM; 20 μM
Incubation Time: 1, 2, 3, and 4 days
Result: Inhibited cell proliferation in a CDK2-dependent manner.
Molecular Weight

501.50

Formula

C24H26F3N7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(OC2=CC=C(NC(NC3=CC(C(F)(F)F)=C(CN4CCN(C)CC4)C=C3)=O)C=C2)=CC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (498.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9940 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.57%

SDS (393 KB)

COA (248 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9940 mL 9.9701 mL 19.9402 mL 49.8504 mL
5 mM 0.3988 mL 1.9940 mL 3.9880 mL 9.9701 mL
10 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9850 mL
15 mM 0.1329 mL 0.6647 mL 1.3293 mL 3.3234 mL
20 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
25 mM 0.0798 mL 0.3988 mL 0.7976 mL 1.9940 mL
30 mM 0.0665 mL 0.3323 mL 0.6647 mL 1.6617 mL
40 mM 0.0499 mL 0.2493 mL 0.4985 mL 1.2463 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9970 mL
60 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
80 mM 0.0249 mL 0.1246 mL 0.2493 mL 0.6231 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
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AUZ 454 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AUZ 454853299-07-7K03861AUZ454AUZ-454K 03861K-03861CDKCyclin dependent kinaseCDK2Caki-1ACHNcellsInhibitorinhibitorinhibit

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