CFI-400437 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CFI-400437 是一种选择性且有效的 polo 样激酶 4 (PLK4) 抑制剂。

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

——

(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.

——

Cell Cycle/DNA Damage

PLK

PLK4

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years