2. PROTAC Epigenetics Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. PROTACs Aurora Kinase E1/E2/E3 Enzyme
  4. CCT400028

CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-W671452); Black: linker).

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

CCT400028

CCT400028 Chemical Structure

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

CCT400028 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma[1]. (Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-W671452); Black: linker).

IC50 & Target

Cereblon

 

Aurora A

71 nM (Kd)

Aurora B

2100 nM (Kd)

Aurora C

>10 μM (Kd)

In Vitro

CCT400028 (0.001-10 μM; 0-24 h) shows no hook effect, potently degrades Aurora A in MV4-11 human pediatric leukemia cells, with a DC50 of 29 nM at 6 h and a DCmax of 85%; it also induces potent and sustained (24 h) Aurora A degradation in human pediatric neuroblastoma Kelly cells[1].
The Aurora A degradation activity of CCT400028 (1 μM; 4 h) in human pediatric neuroblastoma Kelly cells can be blocked by proteasome function inhibitors, Cullin ring ligase activity inhibitors, CRBN-binding inhibitors, and Aurora A-binding inhibitors (inhibitors require 2 h of pre-treatment)[1].
CCT400028 (0.01-10 μM; 72 h) inhibits the viability of human pediatric leukemia cells MV4-11, with a GI50 of 310 nM[1].

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

CCT400028 Related Antibodies

Western Blot Analysis[1]

Cell Line: Kelly human pediatric neuroblastoma cells
Concentration: 0.001-10 μM
Incubation Time: 4 h; 24 h
Result: Induced robust, sustained Aurora A depletion at both 4 h and 24 h. Reduced Aurora A levels to near-background at concentrations ≥0.1 μM by 4 h, and maintained this depletion at 24 h. Showed no hook effect across the tested concentration range.

Western Blot Analysis[1]

Cell Line: Kelly human pediatric neuroblastoma cells
Concentration: 1 μM (CCT400028; preceded by 2 h pre-incubation with 10 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062), 10 μM CC220 (HY-101291), 0.25-5 μM Alisertib (HY-10971))
Incubation Time: 4 h (CCT400028 co-treatment; 2 h pre-incubation with inhibitors)
Result: Induced robust, sustained Aurora A depletion at both 4 h and 24 h.
Showed no hook effect across the tested concentration range.
Induced Aurora A degradation that was completely blocked by pretreatment with the proteasome inhibitor MG132 (HY-13259) and the neddylation inhibitor MLN4924 (HY-70062).
Induced Aurora A degradation that was inhibited by pretreatment with the CRBN ligand CC220 (HY-101291) and the Aurora A inhibitor Alisertib (HY-10971).
Molecular Weight

878.39

Formula

C47H49ClFN7O7
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC(CCN1C2=CC=C(C=C2)OCCCCCOCCCCCNC(C3=CC=C(C=C3OC)NC4=NC5=C(C=N4)CN=C(C6=C(C=CC=C6OC)F)C7=CC(Cl)=CC=C57)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (113.84 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 1.1384 mL 5.6922 mL 11.3845 mL
5 mM 0.2277 mL 1.1384 mL 2.2769 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1384 mL 5.6922 mL 11.3845 mL 28.4612 mL
5 mM 0.2277 mL 1.1384 mL 2.2769 mL 5.6922 mL
10 mM 0.1138 mL 0.5692 mL 1.1384 mL 2.8461 mL
15 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
20 mM 0.0569 mL 0.2846 mL 0.5692 mL 1.4231 mL
25 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1384 mL
30 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
40 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7115 mL
50 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
60 mM 0.0190 mL 0.0949 mL 0.1897 mL 0.4744 mL
80 mM 0.0142 mL 0.0712 mL 0.1423 mL 0.3558 mL
100 mM 0.0114 mL 0.0569 mL 0.1138 mL 0.2846 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CCT400028 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:

CCT400028CCT 400028CCT-400028PROTACsAurora KinaseE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseneuroblastomaE3 ubiquitin ligasecereblonproteasomal degradationCRBNAURKAleukemiagliomapediatric tumor cellsAurora AInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CCT400028
Cat. No.:
HY-181311
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.