产品
编 号:F090614
分子式:C29H30Cl2N6O2
分子量:565.49
产品类型
结构图
CAS No: 1247000-76-5
联系客服
产品详情
生物活性:
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.
体内研究:
(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.