2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Neuronal Signaling Apoptosis
  3. Polo-like Kinase (PLK) Trk Receptor Apoptosis
  4. CZS-241

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

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

CZS-241 Chemical Structure

CZS-241 Chemical Structure

CAS No. : 3016297-55-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

CZS-241 Related Antibodies

Top Publications Citing Use of Products

View All Polo-like Kinase (PLK) Isoform Specific Products:

View All Isoforms
PLK1 PLK2 PLK3 PLK4

View All Trk Receptor Isoform Specific Products:

View All Isoforms
TrkA TrkB TrkC Trk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines[1].

IC50 & Target[1]

PLK4

2.6 nM (IC50)

TrkA

2.74 μM (IC50)

In Vitro

CZS-241 inhibits cell proliferation of chronic myeloid leukemia (CML) cell lines K562 and KU-812 with IC50s of 0.096 μM and 0.25 μM, respectively. CZS-241 has little effect on normal cells including HUVECs and L02[1].
CZS-241 (10 μM; 0-120 min) exhibits 31.5 min of half-life t1/2 and 41.8 μL/min/kg of CLint in human liver microsomal[1].
CZS-241 (0.3 μM, 1 μM, 3 μM; 48 h) arrests cell cycle at S/G2 phase, induces apoptosis in K562 CML cells[1].
CZS-241 (0.03-0.3 μM) inhibits the phosphorylation of PLK4, increases the FBXW5 expression level but decreases the SAS-6 expression level in K562 cells[1].

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

CZS-241 Related Antibodies

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, and 3 μM
Incubation Time:
Result: Showed insignificant effect on PLK4 relative expression, but decreased the expression of SAS-6 dose-dependently.
Increased the expression level of FBXW5.
In Vivo

CZS-241 (30 mg/kg; p.o.; single dose) shows over 4 h of half-life and 70.8% bioavailability in mice[1].
CZS-241 (20 mg/kg/day; p.o.; 21 days) suppresses tumor progression significantly in K562 cells xenograft mouse model[1].
CZS-241 (200 mg/kg; p.o.; single dose) has no obvious signs of toxicity in heart, liver, spleen, lungs, and kidneys of mice, within 7 days of monitoring[1].

Pharmacokinetic Analysis in mice[1]

Route Dose (mg/kg) AUClast (ng·h/mL) AUCINF_obs (ng·h/mL) t1/2 (h) Tmax (h) Cmax (ng/mL) Clobs (L·h/kg) Vss_obs (mL/kg) MRTINF_obs (h) F (%)
i.v. 3 727 739 2.15 / / 68.7 12615 1.28 70.8
p.o. 30 5177 5231 4.13 0.67 1880 / / 3.87 /

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

Animal Model: K562 cells xenograft mouse model[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: PO; once daily, for continuous 21 days
Result: Showed potent antitumor activity with mouse body weight increased normally. Exhibited tumor growth inhibition (TGI) rate of 56.4% at 20 mg/kg/day dosage.
Molecular Weight

551.98

Formula

C26H24ClF2N9O
CAS No.
SMILES

FC1=CC=C(C=C1NC(C2=C(C=CC(CNC3=NC4=C(C(NC5=NNC(C)=C5)=N3)C=NN4C(C)C)=C2)Cl)=O)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

CZS-241 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

CZS-2413016297-55-2CZS241CZS 241Polo-like Kinase (PLK)Trk ReceptorApoptosisTropomyosin related kinase receptor Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CZS-241
Cat. No.:
HY-149912
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 (0 KB) Français - FR (0 KB) Deutsch - DE (0 KB) Norwegian - NO (0 KB) Español - ES (0 KB) Swedish - SV (0 KB)

Request for HNMR Report

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