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.

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CZS-241 Chemical Structure

CZS-241 Chemical Structure

CAS No. : 3016297-55-2

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CZS-241 Related Antibodies

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PLK1 PLK2 PLK3 PLK4

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TrkA TrkB TrkC Trk

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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
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CZS-241 Related Classifications

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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

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