CZS-241 | PLK4 inhibitor | Probechem Biochemicals

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Chemical Structure : CZS-241

CZS-241 (PLK4 inhibitor B43)

Catalog No.: PC-25890Not For Human Use, Lab Use Only.

CZS-241 is a potent, selective PLK4 inhibitor with IC50 of 2.6 nM for PLK4, >1000-fold selective over TRKA.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CZS-241 is a potent, selective PLK4 inhibitor with IC50 of 2.6 nM for PLK4, >1000-fold selective over TRKA.
CZS-241 potently inhibits chronic myeloid leukemia (CML) cell lines K562 (IC50 =0.096 μM) and KU-812 (IC50 = 0.25 μM).
CZS-241 has high selectivity to other members of PLK family (PLK1-3), high homology kinases (Aurora B and TRK A/B).
CZS-241 exhibited promising in vivo efficacy in the chronic myeloid leukemia (CML) K562 cells xenograft mouse model.

Physicochemical Properties

M.Wt	551.99
Formula	C26H24ClF2N9O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Chloro-N-(2,5-difluorophenyl)-5-(((1-isopropyl-4-((5-methyl-1H-pyrazol-3-yl)amino)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)methyl)benzamide

References

1. Yin Sun, et al. J Med Chem. 2023 Feb 23;66(4):2396-2421.

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CZS-241 (PLK4 inhibitor B43)

Biological Activity

Physicochemical Properties

References

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