CFI-400437 dihydrochloride

Research use only, not for human use.

CFI-400437 is a selective and potent polo-like kinase 4 (PLK4) inhibitor.

CFI-400437 is a selective and potent polo-like kinase 4 (PLK4) inhibitor.

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(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth.The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng?h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%. Animal Model:6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model)Dosage:25 mg/kg Administration:Intraperitoneal injection; daily for 21 days Result:Effective in a mouse xenograft model of tumor growth.In this study, (1E)-CFI-400437 is weighed and suspended in PEG400:water (30:70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at ?20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose.

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Cell Cycle/DNA Damage

PLK

PLK4

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1247000-76-5

565.5

C29H30Cl2N6O2

>98% (HPLC)

DMSO:5 mM

CN1CCN(CC1)C2=NC=C(C=C2)/C=C/C3=C4C=CC(=CC5=C(NC6=C5C=C(C=C6)OC)O)C=C4N=N3.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years