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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- CAS No.: 3016297-55-2
- Formule: C26H24ClF2N9O
- Masse moléculaire:551.98
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PLK4 2.6 nM (IC50) |
TrkA 2.74 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| K562 | IC50 |
0.096 μM
Compound: B43; CZS-241
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Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 5 days
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 5 days
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[PMID: 36734825] |
| KU812 cell line | IC50 |
0.25 μM
Compound: B43; CZS-241
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Antiproliferative activity against human KU812 cells assessed as inhibition of cell growth incubated for 5 days
Antiproliferative activity against human KU812 cells assessed as inhibition of cell growth incubated for 5 days
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[PMID: 36734825] |
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.
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Cell Line:K562 cells
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Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, and 3 μM
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Incubation Time:
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Result:Showed insignificant effect on PLK4 relative expression, but decreased the expression of SAS-6 dose-dependently.
Increased the expression level of FBXW5.
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.
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Animal Model:K562 cells xenograft mouse model[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:PO; once daily, for continuous 21 days
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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.
Chemical Information
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CAS No. 3016297-55-2
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Masse moléculaire 551.98
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Formule C26H24ClF2N9O
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CZS-241 Related Classifications
HY-149912 Related Classifications
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